76809-55-7Relevant academic research and scientific papers
Synthesis and evaluation of moxifloxacin derivatives for effects on proliferation and apoptosis of NCI-H1299 cells
Yu, Fangmiao,Zhang, Zhuangwei,Li, Wei,Tian, Hengqun,Xu, Jun,Bao, Yongzhong
, (2020)
Eight novel moxifloxacin (MXF) derivatives 4a-h were synthesized by functional modification of the N-5-Aza ring. Their growth inhibitory activities on human non-small lung cancer cell NCI-H1299 and A549 were evaluated by the MTT colorimetric assay. Based on the half inhibitory concentration (IC50) values, we determined that compounds 4b was the most efficacious derivative (IC50 = 2.56 ± 0.07 μM for NCI-H1299 and IC50 = 13.69 ± 0.70 μM for A549, respectively) that inhibited the proliferation of NCI-H1299 cells. Of these, Compound 4b (1 – cyclopropyl – 6 – fluoro – 8 – methoxy – 4 – oxo – 7 – ((4aS,7aS) – 1 – (2 – oxo – 2 – (p – tolylamino) ethyl) hexahydro – 1H – pyrrolo [3,4-b] pyridine – 6(2H)-yl) – 1,4 – dihydroquinoline – 3-carboxylic acid) showed good potency against the growth of NCI-H1299 cells and also selectivity on HUVEC cells (IC50 > 500 μM). The dose-response relationship of the characteristic morphological changes of NCI-H1299 cells induced by Compound 4b was confirmed by AO/EB fluorescent staining. Furthermore, Compound 4b triggered apoptosis of NCI-H1299 in a concentration-dependent manner and arrested cells in the G0/G1 phase. These data indicate that the N-(p-tolyl)propanamide functionalized N-5-Aza ring of moxifloxacin may be a promising lead compound and candidate for the development of new agents against non-small-cell lung cancer.
Design and synthesis of novel 4'-demethyl-4-deoxypodophyllotoxin derivatives as potential anticancer agents
Zhu, Xiong,Fu, Junjie,Tang, Yan,Gao, Yuan,Zhang, Shijin,Guo, Qinglong
supporting information, p. 1360 - 1364 (2016/02/23)
A group of podophyllotoxin (PPT) derivatives (7a-j) were synthesized by conjugating aryloxyacetanilide moieties to the 4'-hydroxyl of 4'-demethyl-4-deoxypodophyllotoxin (DDPT), and their anticancer activity was evaluated. It was found that the most potent compound 7d inhibited the proliferation of three cancer cell lines with sub to low micromolar IC50 values. Furthermore, it was demonstrated that 7d induced cell cycle arrest in G2/M phase in MGC-803 cells, and regulated the expression of cell cycle check point proteins, such as cyclin A, cyclin B, CDK1, cdc25c, and p21. Finally, 4 mg/kg of 7d reduced the weights and volumes of HepG2 xenografts in mice. Our findings suggest that 7d might be a potential anticancer agent.
Synthesis and in vitro antitumor activity of novel scopoletin derivatives
Liu, Wukun,Hua, Jie,Zhou, Jinpei,Zhang, Huibin,Zhu, Haiyang,Cheng, Yanhua,Gust, Ronald
scheme or table, p. 5008 - 5012 (2012/08/28)
Twenty scopoletin derivatives were developed by a systematic combinatorial chemical approach and their chemical structures were confirmed by MS, IR, 1H NMR spectra and elemental analysis. Primary screening against mammary (MCF-7 and MDA-MB 231) and colon (HT-29) carcinoma cells indicated that five compounds (8d, 8g, 8j, 11b and 11g) displayed high antitumor potencies with IC50 values below 20 μM whereas scopoletin showed IC50 values above 100 μM. Moreover, the most promising compound 11g was more active than 5-fluorouracil. These results clearly indicated that the modification of the scopoletin structure could greatly increase its antitumor activity in vitro.
Synthesis of 1-[N-(aryl)methylcarbamoyl]-1, 10-phenanthrolinium iodides with potential biological activity
Dumitra?cu, Florea,Drǎghici, Constantin,Caira, Mino R.,Bǎdoiu, Andrei,Barbu, Loredana
, p. 19 - 23 (2007/10/03)
1-[N-(aryl)methylcarbamoyl]-1,10-phenanthrolinium iodides 10b-g were obtained by the reaction between N-aryl-2-iodoacetamides 9b-g and 1,10-phenanthroline. Also, the primary amide 10a was prepared by quaternization of 1,10-phenanthroline with iodoacetamid
