Jiabin Li
Current Organizations / Institutes
The organizations/institutes from the scholar's latest article
Jiabin Li has a total of 8 co-authors. Here are the top co-authors by number of shared publications:
- Hongbin Sun
China Pharmaceutical University
1 shared publication Jun Xia
Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China
1 shared publication- Kejiang Lin
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China
1 shared publication - Xiaowen Xue
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 211198, China
1 shared publication Yuchen He
Department of Medicinal Chemistry China Pharmaceutical University 24 Tong Jia Xiang 210009 Nanjing China
1 shared publication- Yunlong Lu
China Pharmaceut Univ, Dept Med Chem, 24 Tong Jia Xiang, Nanjing 210009, Jiangsu, Peoples R China
1 shared publication
Latest Publications
- 24 January 2018
- Published by Wiley in European Journal of Organic Chemistry
- Vol. 2018 (4) , 477-484
Stereoselective Synthesis and Biological Evaluation of ent‐Asperolide C and its Analogues
A stereoselective synthesis of ent‐asperolide C and its analogues is described. A chiral‐pool approach was used with a linear sequence of 10 steps, starting from readily available and inexpensive andrographolide. The approach features the construction of a five‐membered lactone skeleton with suitable chiral centres from andrographolide through diastereoselective epoxidation of the exocyclic double bond, and tandem oxidative cleavage of the C‐14=C‐15 double bond and subsequent epoxide ring opening. The stereochemistry of 8 was established by X‐ray crystallographic analysis. Four analogues of ent‐asperolide C were synthesized, and their biological activities were evaluated against A539 and HeLa cell lines. Compound 12 was found to show a weak to moderate antiproliferation effect against both cell lines.
- 24 January 2018
- Published by Wiley in European Journal of Organic Chemistry
- Vol. 2018 (4) , 477-484
Stereoselective Synthesis and Biological Evaluation of ent‐Asperolide C and its Analogues
A stereoselective synthesis of ent‐asperolide C and its analogues is described. A chiral‐pool approach was used with a linear sequence of 10 steps, starting from readily available and inexpensive andrographolide. The approach features the construction of a five‐membered lactone skeleton with suitable chiral centres from andrographolide through diastereoselective epoxidation of the exocyclic double bond, and tandem oxidative cleavage of the C‐14=C‐15 double bond and subsequent epoxide ring opening. The stereochemistry of 8 was established by X‐ray crystallographic analysis. Four analogues of ent‐asperolide C were synthesized, and their biological activities were evaluated against A539 and HeLa cell lines. Compound 12 was found to show a weak to moderate antiproliferation effect against both cell lines.
- 12 July 2011
- Published by Springer Nature in Journal of Molecular Modeling
- Vol. 18 (4) , 1299-1311
Insights into ETA subtype selectivity of benzodiazepine endothelin receptor antagonists by 3D-QSAR approaches
ETA subtype selective antagonists constitute a novel and potentially important class of agents for the treatment of pulmonary hypertension, heart failure, and other pathological conditions. In this paper, 60 benzodiazepine derivatives displaying potent activities against ETA and ETB subtypes of endothelin receptor were selected to establish the 3D-QSAR models using CoMFA and CoMSIA approaches. These models show excellent internal predictability and consistency, external validation using test-set 19 compounds yields a good predictive power for antagonistic potency. Statistical parameters of models were obtained with CoMFA-ETA (q 2 = 0.787, r 2 = 0.935, r 2 pred = 0.901), CoMFA-ETB (q 2 = 0.842, r 2 = 0.984, r 2 pred = 0.941), CoMSIA-ETA (q 2 = 0.762, r 2 = 0.971, r 2 pred = 0.958) and CoMSIA-ETB (q 2 = 0.771, r 2 = 0.974, r 2 pred = 0.953) respectively. Field contour maps (CoMFA and CoMSIA) corresponding to the ETA and ETB subtypes reflects the characteristic similarities and differences between these types. The results of this paper provide valuable information to facilitate structural modifications of the title compounds to increase the inhibitory potency and subtype selectivity of endothelin receptor.
- 12 July 2011
- Published by Springer Nature in Journal of Molecular Modeling
- Vol. 18 (4) , 1299-1311
Insights into ETA subtype selectivity of benzodiazepine endothelin receptor antagonists by 3D-QSAR approaches
ETA subtype selective antagonists constitute a novel and potentially important class of agents for the treatment of pulmonary hypertension, heart failure, and other pathological conditions. In this paper, 60 benzodiazepine derivatives displaying potent activities against ETA and ETB subtypes of endothelin receptor were selected to establish the 3D-QSAR models using CoMFA and CoMSIA approaches. These models show excellent internal predictability and consistency, external validation using test-set 19 compounds yields a good predictive power for antagonistic potency. Statistical parameters of models were obtained with CoMFA-ETA (q 2 = 0.787, r 2 = 0.935, r 2 pred = 0.901), CoMFA-ETB (q 2 = 0.842, r 2 = 0.984, r 2 pred = 0.941), CoMSIA-ETA (q 2 = 0.762, r 2 = 0.971, r 2 pred = 0.958) and CoMSIA-ETB (q 2 = 0.771, r 2 = 0.974, r 2 pred = 0.953) respectively. Field contour maps (CoMFA and CoMSIA) corresponding to the ETA and ETB subtypes reflects the characteristic similarities and differences between these types. The results of this paper provide valuable information to facilitate structural modifications of the title compounds to increase the inhibitory potency and subtype selectivity of endothelin receptor.