Month: September 2021

Application In Synthesis of (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. Lei, M; Feng, HY; Bai, EH; Zhou, H; Wang, J; Qin, YR; Zhang, HY; Wang, XY; Liu, ZG; Hai, O; Liu, J; Zhu, YQ in [Lei, Meng; Feng, Huayun] Nanjing Forestry Univ, Coll Sci, 159 Longpan Rd, Nanjing 210037, Jiangsu, Peoples R China; [Bai, Enhe; Zhou, Hui; Zhang, Haoyang; Wang, Xueyuan; Zhu, Yongqiang] Nanjing Normal Univ, Coll Life Sci, 1 Wenyuan Rd, Nanjing 210037, Jiangsu, Peoples R China; [Wang, Jia; Liu, Zhaogang; Hai, Ou; Liu, Jia] Jiangsu Chia Tai Fenghai Pharmaceut Co Ltd, 9 Weidi Rd, Nanjing 210046, Jiangsu, Peoples R China; [Qin, Yanru] Qilu Univ Technol, Shandong Acad Sci, Sch Bioengn, 3501 Daxue Rd, Jinan 250353, Shandong, Peoples R China published Discovery of a novel dipeptidyl boronic acid proteasome inhibitor for the treatment of multiple myeloma and triple- negative breast cancer in 2019, Cited 30. The Name is (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. Through research, I have a further understanding and discovery of 179324-87-9.

A series of novel dipeptidyl boronic acid compounds were designed, synthesized and biologically investigated for the inhibition of the 5 subunit of 20S proteasome and several compounds showed high activities with IC50 values of less than 10 nM. Some of these compounds potently inhibited the multiple myeloma (MM) cancer cell lines with IC50 values of less than 10 nM. It was reported that the inhibition of both 2 and 5 subunits strongly increased the cytotoxicity of proteasome inhibitors in solid tumor cells, so some of the compounds were evaluated for the inhibition of the 2 subunit and the solid tumor triple-negative breast cancer cell line MDA-MB-231. The results showed that three compounds were active for both the 2 subunit and the triple-negative breast cancer cell line MDA-MB-231. The in vivo pharmacokinetic results showed that compound 8t had good biological parameters for both ig and iv administrations. An in vivo pharmacodynamic experiment showed that compound 8t inhibited the 5 subunit in whole blood more greatly than the marketed MLN9708 with the same dose at different time periods. A pathological analysis indicated that the injection of compound 8t in the tumor of a triple-negative breast cancer xenograft mice model led to tumor cell necrosis, nucleus condensation, deep staining, cell fragmentation, dissolution and neutrophil infiltration compared with the control group. The data in hand showed that compound 8t might be an effective candidate for the treatment of both MM and triple-negative breast cancer.

About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Lei, M; Feng, HY; Bai, EH; Zhou, H; Wang, J; Qin, YR; Zhang, HY; Wang, XY; Liu, ZG; Hai, O; Liu, J; Zhu, YQ or concate me.. Application In Synthesis of (R)-BoroLeu-(+)-Pinanediol trifluoroacetate

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem

In 2020 J MED CHEM published article about AUREUS STRESS TOLERANCE; STAPHYLOCOCCUS-AUREUS; PROTEASE; INSIGHTS; CLEAVAGE; REVEAL; ROLES in [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Sang, Zitai] Luoyang Normal Univ, Inst Life Sci, Luoyang 471934, Henan, Peoples R China in 2020, Cited 53. The Name is (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. Through research, I have a further understanding and discovery of 179324-87-9. SDS of cas: 179324-87-9

Caseinolytic protease P (ClpP) is considered as a promising target for the treatment of Staphylococcus aureus infections. In an unbiased screen of 2632 molecules, a peptidomimetic boronate, MLN9708, was found to be a potent suppressor of SaClpP function. A time-saving and cost-efficient strategy integrating in silico position scanning, multistep miniaturized synthesis, and bioactivity testing was deployed for optimization of this hit compound and led to fast exploration of structure-activity relationships. Five of 150 compounds from the miniaturized synthesis exhibited improved inhibitory activity. Compound 43Hf was the most active inhibitor and showed reversible covalent binding to SaClpP while did not destabilize the tetradecameric structure of SaClpP. The crystal structure of 43Hf-SaClpP complex provided mechanistic insight into the covalent binding mode of peptidomimetic boronate and SaClpP. Furthermore, 43Hf could bind endogenous ClpP in S. aureus cells and exhibited significant efficacy in attenuating S. aureus virulence in vitro and in vivo.

SDS of cas: 179324-87-9. About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Ju, Y; He, LH; Zhou, YZ; Yang, T; Sun, K; Song, R; Yang, Y; Li, CW; Sang, ZT; Bao, R; Luo, YF or concate me.

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem

In 2020 J MED CHEM published article about AUREUS STRESS TOLERANCE; STAPHYLOCOCCUS-AUREUS; PROTEASE; INSIGHTS; CLEAVAGE; REVEAL; ROLES in [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Sang, Zitai] Luoyang Normal Univ, Inst Life Sci, Luoyang 471934, Henan, Peoples R China in 2020, Cited 53. The Name is (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. Through research, I have a further understanding and discovery of 179324-87-9. Category: naphthyridines

Caseinolytic protease P (ClpP) is considered as a promising target for the treatment of Staphylococcus aureus infections. In an unbiased screen of 2632 molecules, a peptidomimetic boronate, MLN9708, was found to be a potent suppressor of SaClpP function. A time-saving and cost-efficient strategy integrating in silico position scanning, multistep miniaturized synthesis, and bioactivity testing was deployed for optimization of this hit compound and led to fast exploration of structure-activity relationships. Five of 150 compounds from the miniaturized synthesis exhibited improved inhibitory activity. Compound 43Hf was the most active inhibitor and showed reversible covalent binding to SaClpP while did not destabilize the tetradecameric structure of SaClpP. The crystal structure of 43Hf-SaClpP complex provided mechanistic insight into the covalent binding mode of peptidomimetic boronate and SaClpP. Furthermore, 43Hf could bind endogenous ClpP in S. aureus cells and exhibited significant efficacy in attenuating S. aureus virulence in vitro and in vivo.

Category: naphthyridines. About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Ju, Y; He, LH; Zhou, YZ; Yang, T; Sun, K; Song, R; Yang, Y; Li, CW; Sang, ZT; Bao, R; Luo, YF or concate me.

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem

I found the field of Chemistry very interesting. Saw the article Discovery of a novel dipeptidyl boronic acid proteasome inhibitor for the treatment of multiple myeloma and triple- negative breast cancer published in 2019. Product Details of 179324-87-9, Reprint Addresses Lei, M (corresponding author), Nanjing Forestry Univ, Coll Sci, 159 Longpan Rd, Nanjing 210037, Jiangsu, Peoples R China.; Zhu, YQ (corresponding author), Nanjing Normal Univ, Coll Life Sci, 1 Wenyuan Rd, Nanjing 210037, Jiangsu, Peoples R China.. The CAS is 179324-87-9. Through research, I have a further understanding and discovery of (R)-BoroLeu-(+)-Pinanediol trifluoroacetate

A series of novel dipeptidyl boronic acid compounds were designed, synthesized and biologically investigated for the inhibition of the 5 subunit of 20S proteasome and several compounds showed high activities with IC50 values of less than 10 nM. Some of these compounds potently inhibited the multiple myeloma (MM) cancer cell lines with IC50 values of less than 10 nM. It was reported that the inhibition of both 2 and 5 subunits strongly increased the cytotoxicity of proteasome inhibitors in solid tumor cells, so some of the compounds were evaluated for the inhibition of the 2 subunit and the solid tumor triple-negative breast cancer cell line MDA-MB-231. The results showed that three compounds were active for both the 2 subunit and the triple-negative breast cancer cell line MDA-MB-231. The in vivo pharmacokinetic results showed that compound 8t had good biological parameters for both ig and iv administrations. An in vivo pharmacodynamic experiment showed that compound 8t inhibited the 5 subunit in whole blood more greatly than the marketed MLN9708 with the same dose at different time periods. A pathological analysis indicated that the injection of compound 8t in the tumor of a triple-negative breast cancer xenograft mice model led to tumor cell necrosis, nucleus condensation, deep staining, cell fragmentation, dissolution and neutrophil infiltration compared with the control group. The data in hand showed that compound 8t might be an effective candidate for the treatment of both MM and triple-negative breast cancer.

Product Details of 179324-87-9. About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Lei, M; Feng, HY; Bai, EH; Zhou, H; Wang, J; Qin, YR; Zhang, HY; Wang, XY; Liu, ZG; Hai, O; Liu, J; Zhu, YQ or concate me.

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem

An article Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers in Vitro and in Vivo WOS:000526404600023 published article about AUREUS STRESS TOLERANCE; STAPHYLOCOCCUS-AUREUS; PROTEASE; INSIGHTS; CLEAVAGE; REVEAL; ROLES in [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Ju, Yuan; He, Lihui; Zhou, Yuanzheng; Yang, Tao; Sun, Ke; Song, Rao; Yang, Yang; Li, Chengwei; Bao, Rui; Luo, Youfu] Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China; [Sang, Zitai] Luoyang Normal Univ, Inst Life Sci, Luoyang 471934, Henan, Peoples R China in 2020, Cited 53. The Name is (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. Through research, I have a further understanding and discovery of 179324-87-9. Computed Properties of C17H29BF3NO4

Caseinolytic protease P (ClpP) is considered as a promising target for the treatment of Staphylococcus aureus infections. In an unbiased screen of 2632 molecules, a peptidomimetic boronate, MLN9708, was found to be a potent suppressor of SaClpP function. A time-saving and cost-efficient strategy integrating in silico position scanning, multistep miniaturized synthesis, and bioactivity testing was deployed for optimization of this hit compound and led to fast exploration of structure-activity relationships. Five of 150 compounds from the miniaturized synthesis exhibited improved inhibitory activity. Compound 43Hf was the most active inhibitor and showed reversible covalent binding to SaClpP while did not destabilize the tetradecameric structure of SaClpP. The crystal structure of 43Hf-SaClpP complex provided mechanistic insight into the covalent binding mode of peptidomimetic boronate and SaClpP. Furthermore, 43Hf could bind endogenous ClpP in S. aureus cells and exhibited significant efficacy in attenuating S. aureus virulence in vitro and in vivo.

About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Ju, Y; He, LH; Zhou, YZ; Yang, T; Sun, K; Song, R; Yang, Y; Li, CW; Sang, ZT; Bao, R; Luo, YF or concate me.. Computed Properties of C17H29BF3NO4

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem

Formula: C17H29BF3NO4. I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers in Vitro and in Vivo published in 2020, Reprint Addresses Bao, R; Luo, YF (corresponding author), Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.; Bao, R; Luo, YF (corresponding author), Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.. The CAS is 179324-87-9. Through research, I have a further understanding and discovery of (R)-BoroLeu-(+)-Pinanediol trifluoroacetate.

Caseinolytic protease P (ClpP) is considered as a promising target for the treatment of Staphylococcus aureus infections. In an unbiased screen of 2632 molecules, a peptidomimetic boronate, MLN9708, was found to be a potent suppressor of SaClpP function. A time-saving and cost-efficient strategy integrating in silico position scanning, multistep miniaturized synthesis, and bioactivity testing was deployed for optimization of this hit compound and led to fast exploration of structure-activity relationships. Five of 150 compounds from the miniaturized synthesis exhibited improved inhibitory activity. Compound 43Hf was the most active inhibitor and showed reversible covalent binding to SaClpP while did not destabilize the tetradecameric structure of SaClpP. The crystal structure of 43Hf-SaClpP complex provided mechanistic insight into the covalent binding mode of peptidomimetic boronate and SaClpP. Furthermore, 43Hf could bind endogenous ClpP in S. aureus cells and exhibited significant efficacy in attenuating S. aureus virulence in vitro and in vivo.

About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Ju, Y; He, LH; Zhou, YZ; Yang, T; Sun, K; Song, R; Yang, Y; Li, CW; Sang, ZT; Bao, R; Luo, YF or concate me.. Formula: C17H29BF3NO4

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem

I found the field of Chemistry very interesting. Saw the article Discovery of a novel dipeptidyl boronic acid proteasome inhibitor for the treatment of multiple myeloma and triple- negative breast cancer published in 2019. Name: (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, Reprint Addresses Lei, M (corresponding author), Nanjing Forestry Univ, Coll Sci, 159 Longpan Rd, Nanjing 210037, Jiangsu, Peoples R China.; Zhu, YQ (corresponding author), Nanjing Normal Univ, Coll Life Sci, 1 Wenyuan Rd, Nanjing 210037, Jiangsu, Peoples R China.. The CAS is 179324-87-9. Through research, I have a further understanding and discovery of (R)-BoroLeu-(+)-Pinanediol trifluoroacetate

A series of novel dipeptidyl boronic acid compounds were designed, synthesized and biologically investigated for the inhibition of the 5 subunit of 20S proteasome and several compounds showed high activities with IC50 values of less than 10 nM. Some of these compounds potently inhibited the multiple myeloma (MM) cancer cell lines with IC50 values of less than 10 nM. It was reported that the inhibition of both 2 and 5 subunits strongly increased the cytotoxicity of proteasome inhibitors in solid tumor cells, so some of the compounds were evaluated for the inhibition of the 2 subunit and the solid tumor triple-negative breast cancer cell line MDA-MB-231. The results showed that three compounds were active for both the 2 subunit and the triple-negative breast cancer cell line MDA-MB-231. The in vivo pharmacokinetic results showed that compound 8t had good biological parameters for both ig and iv administrations. An in vivo pharmacodynamic experiment showed that compound 8t inhibited the 5 subunit in whole blood more greatly than the marketed MLN9708 with the same dose at different time periods. A pathological analysis indicated that the injection of compound 8t in the tumor of a triple-negative breast cancer xenograft mice model led to tumor cell necrosis, nucleus condensation, deep staining, cell fragmentation, dissolution and neutrophil infiltration compared with the control group. The data in hand showed that compound 8t might be an effective candidate for the treatment of both MM and triple-negative breast cancer.

Name: (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Lei, M; Feng, HY; Bai, EH; Zhou, H; Wang, J; Qin, YR; Zhang, HY; Wang, XY; Liu, ZG; Hai, O; Liu, J; Zhu, YQ or concate me.

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem

Name: (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers in Vitro and in Vivo published in 2020, Reprint Addresses Bao, R; Luo, YF (corresponding author), Sichuan Univ, State Key Lab Biotherapy, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.; Bao, R; Luo, YF (corresponding author), Sichuan Univ, Canc Ctr, Collaborat Innovat Ctr Biotherapy, West China Hosp, Chengdu 610041, Peoples R China.. The CAS is 179324-87-9. Through research, I have a further understanding and discovery of (R)-BoroLeu-(+)-Pinanediol trifluoroacetate.

Caseinolytic protease P (ClpP) is considered as a promising target for the treatment of Staphylococcus aureus infections. In an unbiased screen of 2632 molecules, a peptidomimetic boronate, MLN9708, was found to be a potent suppressor of SaClpP function. A time-saving and cost-efficient strategy integrating in silico position scanning, multistep miniaturized synthesis, and bioactivity testing was deployed for optimization of this hit compound and led to fast exploration of structure-activity relationships. Five of 150 compounds from the miniaturized synthesis exhibited improved inhibitory activity. Compound 43Hf was the most active inhibitor and showed reversible covalent binding to SaClpP while did not destabilize the tetradecameric structure of SaClpP. The crystal structure of 43Hf-SaClpP complex provided mechanistic insight into the covalent binding mode of peptidomimetic boronate and SaClpP. Furthermore, 43Hf could bind endogenous ClpP in S. aureus cells and exhibited significant efficacy in attenuating S. aureus virulence in vitro and in vivo.

Name: (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Ju, Y; He, LH; Zhou, YZ; Yang, T; Sun, K; Song, R; Yang, Y; Li, CW; Sang, ZT; Bao, R; Luo, YF or concate me.

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem

Recently I am researching about BIOLOGICAL EVALUATION; 20S PROTEASOME; IN-VITRO; BORTEZOMIB; DESIGN; RESISTANCE; RISK, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21877061]; Natural Science Foundation of Jiangsu ProvinceNatural Science Foundation of Jiangsu Province [BK20171448]; National and Local Joint Engineering Research Center of Biomedical Functional Materials; Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD). Name: (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Lei, M; Feng, HY; Bai, EH; Zhou, H; Wang, J; Qin, YR; Zhang, HY; Wang, XY; Liu, ZG; Hai, O; Liu, J; Zhu, YQ. The CAS is 179324-87-9. Through research, I have a further understanding and discovery of (R)-BoroLeu-(+)-Pinanediol trifluoroacetate

A series of novel dipeptidyl boronic acid compounds were designed, synthesized and biologically investigated for the inhibition of the 5 subunit of 20S proteasome and several compounds showed high activities with IC50 values of less than 10 nM. Some of these compounds potently inhibited the multiple myeloma (MM) cancer cell lines with IC50 values of less than 10 nM. It was reported that the inhibition of both 2 and 5 subunits strongly increased the cytotoxicity of proteasome inhibitors in solid tumor cells, so some of the compounds were evaluated for the inhibition of the 2 subunit and the solid tumor triple-negative breast cancer cell line MDA-MB-231. The results showed that three compounds were active for both the 2 subunit and the triple-negative breast cancer cell line MDA-MB-231. The in vivo pharmacokinetic results showed that compound 8t had good biological parameters for both ig and iv administrations. An in vivo pharmacodynamic experiment showed that compound 8t inhibited the 5 subunit in whole blood more greatly than the marketed MLN9708 with the same dose at different time periods. A pathological analysis indicated that the injection of compound 8t in the tumor of a triple-negative breast cancer xenograft mice model led to tumor cell necrosis, nucleus condensation, deep staining, cell fragmentation, dissolution and neutrophil infiltration compared with the control group. The data in hand showed that compound 8t might be an effective candidate for the treatment of both MM and triple-negative breast cancer.

Name: (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Lei, M; Feng, HY; Bai, EH; Zhou, H; Wang, J; Qin, YR; Zhang, HY; Wang, XY; Liu, ZG; Hai, O; Liu, J; Zhu, YQ or concate me.

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem

Safety of (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. Lei, M; Feng, HY; Bai, EH; Zhou, H; Wang, J; Qin, YR; Zhang, HY; Wang, XY; Liu, ZG; Hai, O; Liu, J; Zhu, YQ in [Lei, Meng; Feng, Huayun] Nanjing Forestry Univ, Coll Sci, 159 Longpan Rd, Nanjing 210037, Jiangsu, Peoples R China; [Bai, Enhe; Zhou, Hui; Zhang, Haoyang; Wang, Xueyuan; Zhu, Yongqiang] Nanjing Normal Univ, Coll Life Sci, 1 Wenyuan Rd, Nanjing 210037, Jiangsu, Peoples R China; [Wang, Jia; Liu, Zhaogang; Hai, Ou; Liu, Jia] Jiangsu Chia Tai Fenghai Pharmaceut Co Ltd, 9 Weidi Rd, Nanjing 210046, Jiangsu, Peoples R China; [Qin, Yanru] Qilu Univ Technol, Shandong Acad Sci, Sch Bioengn, 3501 Daxue Rd, Jinan 250353, Shandong, Peoples R China published Discovery of a novel dipeptidyl boronic acid proteasome inhibitor for the treatment of multiple myeloma and triple- negative breast cancer in 2019, Cited 30. The Name is (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. Through research, I have a further understanding and discovery of 179324-87-9.

A series of novel dipeptidyl boronic acid compounds were designed, synthesized and biologically investigated for the inhibition of the 5 subunit of 20S proteasome and several compounds showed high activities with IC50 values of less than 10 nM. Some of these compounds potently inhibited the multiple myeloma (MM) cancer cell lines with IC50 values of less than 10 nM. It was reported that the inhibition of both 2 and 5 subunits strongly increased the cytotoxicity of proteasome inhibitors in solid tumor cells, so some of the compounds were evaluated for the inhibition of the 2 subunit and the solid tumor triple-negative breast cancer cell line MDA-MB-231. The results showed that three compounds were active for both the 2 subunit and the triple-negative breast cancer cell line MDA-MB-231. The in vivo pharmacokinetic results showed that compound 8t had good biological parameters for both ig and iv administrations. An in vivo pharmacodynamic experiment showed that compound 8t inhibited the 5 subunit in whole blood more greatly than the marketed MLN9708 with the same dose at different time periods. A pathological analysis indicated that the injection of compound 8t in the tumor of a triple-negative breast cancer xenograft mice model led to tumor cell necrosis, nucleus condensation, deep staining, cell fragmentation, dissolution and neutrophil infiltration compared with the control group. The data in hand showed that compound 8t might be an effective candidate for the treatment of both MM and triple-negative breast cancer.

Safety of (R)-BoroLeu-(+)-Pinanediol trifluoroacetate. About (R)-BoroLeu-(+)-Pinanediol trifluoroacetate, If you have any questions, you can contact Lei, M; Feng, HY; Bai, EH; Zhou, H; Wang, J; Qin, YR; Zhang, HY; Wang, XY; Liu, ZG; Hai, O; Liu, J; Zhu, YQ or concate me.

Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem