Delving into the Latest Updates on 南京海光应用化学研究所 with Synapse

概览

疾病领域	数量

血液及淋巴系统疾病	1
免疫系统疾病	1
肿瘤	1

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

DNA	1

关联

1

项与南京海光应用化学研究所相关的药物

Bendamustine Hydrochloride

盐酸苯达莫司汀

靶点

DNA

作用机制

DNA抑制剂

在研机构

Dr. Reddy's Laboratories Ltd. [+18]

原研机构

SymBio Pharmaceuticals Ltd.

在研适应症

弥漫性大B细胞淋巴瘤 [+18]

非在研适应症

急性白血病 [+40]

最高研发阶段批准上市

首次获批国家/地区

美国

首次获批日期2008-03-20

2

项与南京海光应用化学研究所相关的临床试验

CTR20130053 / Recruiting临床2期

注射用盐酸苯达莫司汀治疗利妥昔单抗治疗失败的B细胞惰性淋巴瘤的有效性和安全性的单组、多中心临床试验

评价注射用盐酸苯达莫司汀单药治疗利妥昔单抗治疗失败的B细胞惰性淋巴瘤的有效性和安全性

开始日期-

申办/合作机构

南京海光应用化学研究所

[+1]

CTR20130089 / Active, not recruiting临床1期

注射用盐酸苯达莫司汀药代动力学临床试验方案

研究注射用盐酸苯达莫司汀在非霍奇金淋巴瘤受试者体内的药代动力学过程

开始日期2013-05-22

申办/合作机构

南京海光应用化学研究所

[+1]

100 项与南京海光应用化学研究所相关的临床结果

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0 项与南京海光应用化学研究所相关的专利（医药）

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11

项与南京海光应用化学研究所相关的文献（医药）

2020-05-01·Bioorganic & Medicinal Chemistry Letters

Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold

Article

作者: Sun, Huanliang ; Jia, Jianmin ; Wang, Feidong ; Sun, Min

Two series of novel tricyclic oxazine and oxazepine fused quinazolines have been designed, synthesized and evaluated for their inhibitory activity against EGFR and HER2. Structure-activity relationship (SAR) of these compounds was discussed. From the SAR studies, we found that intramolecular cyclization which possessed a functional Michael acceptor group can enhance the antitumor activities. Compounds 1e and 1h were identified as lead compounds which displayed almost 3-4 times more potent inhibition of EGFR and HER2 than the approved drug lapatinib. The satisfactory physicochemical properties of these compounds were also supported by ACD labs. The results presented here will promote the development of newer dual inhibitors of EGFR and HER2.

2016-10-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs

4区 · 医学

Article

作者: Wang, Feidong ; Zong, Zaiwei ; Chen, Xiangfeng ; Sun, Huanliang ; Zhao, Jun ; Sun, Min ; Han, Jiyong ; Du, Youguo

Two series of novel tricyclic oxazine and oxazepine fused quinazolines have been designed and synthesized. The in vitro antitumor effect of the title compounds was screened on N87, A431, H1975, BT474 and Calu-3 cell lines. Compared to gefitinib and erlotinib, compounds 1a-1h were found to demonstrate more potent antitumor activities. Several derivatives could counteract EGF-induced phosphorylation of EGFR in cells, and their potency was comparable to the reference compounds. Compounds 1a-1f, 1h were chosen for further evaluation of EGFR and HER2 in vitro kinase inhibitory activity. Compounds 1c-1f, 1h effectively inhibited the in vitro kinase activity of EGFR and HER2 with similar efficacy as gefitinib and erlotinib.

2014-02-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: Erlotinib analogs

4区 · 医学

Article

作者: Du, Youguo ; Wang, Feidong ; Kong, Lingsheng ; Sun, Min ; Sun, Huanliang ; Chen, Xiangfeng

Two series of novel tricyclic oxazine and oxazepine fused quinazolines have been designed and synthesized. The in vitro antitumor effect of the title compounds was screened on N87, A431, H1975, BT474 and Calu-3 cell lines. Compared to erlotinib and gefitinib, compounds 1a-1h were found to demonstrate more potent antitumor activities. Several derivatives could counteract EGF-induced phosphorylation of EGFR in cells, and their potency was comparable to the reference compounds. Compounds 1a-1h were chosen for further evaluation of EGFR and HER2 in vitro kinase inhibitory activity. Compounds 1b-1f, 1h effectively inhibited the in vitro kinase activity of EGFR and HER2 with similar efficacy as erlotinib and gefitinib.

100 项与南京海光应用化学研究所相关的药物交易

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100 项与南京海光应用化学研究所相关的转化医学

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