703-80-0Relevant articles and documents
Synthesis, biological evaluation and molecular modeling of imidazo[1,2-a]pyridine derivatives as potent antitubulin agents
Liu, Jin,Zuo, Daiying,Jing, Tongfei,Guo, Ming,Xing, Lingyun,Zhang, Wenyu,Zhao, Jianwen,Shen, Jiwei,Gong, Ping,Zhang, Dajun,Zhai, Xin
, p. 4088 - 4099 (2017)
Two series of novel 5,7-diarylimidazo[1,2-a]pyridine-8-carbonitrile derivatives (3a–3q and 7a–7n) were designed by modification of CA-4 pharmacophore to develop colchicine targeted antitubulin agents. All compounds were efficiently synthesized and evaluated for their cytotoxicity against five selected cancer cell lines (HT-29, H460, A549, MKN-45 and SMMC-7721) which got an insight in structure and activity relationships (SARs). Several molecules (7e, 7f, 7h–7j and 7m) were disclosed to exhibit promising antiproliferative activity with IC50 values in double-digit nanomolar degree. Optimization toward these compounds led to the discovery of a promising lead 7e, which showed noteworthy potency with IC50 value ranging from 0.01 to 3.2?μM superior to CA-4 and Crolibulin. Importantly, immunofluorescence staining and colchcine competitive binding assay revealed that microtubule dynamics was disrupted by 7e by binding at the colchicine site of tubulin. Moreover, molecular docking studies suggested the binding of this mimic at colchcine-binding site is similar to Crolibulin, as was in conformity with the observed SARs for these compounds.
Natural product Pimprinine derivative as well as preparation method and application thereof
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Paragraph 0047, (2021/07/31)
The invention discloses a Pimprinine derivative as shown in a formula III in the description. The invention also discloses a preparation method of the Pimprinine derivative, and a series of Pimprinine derivatives are synthesized by taking Pimprinine as a lead, combining the structural characteristics of Pimprinine, taking cheap and easily available indole as a raw material, modifying and transforming different sites of a framework structure of the indole and introducing different substituent groups. The Pimprinine derivative disclosed by the invention has good bactericidal activity, shows efficient and/or broad-spectrum bactericidal activity, and can be applied to crop diseases caused by fungi, bacteria and viruses.
Sulfonimide photo-acid generator with high acid yield
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Paragraph 0176-0181, (2021/03/30)
The invention discloses a sulfonimide photo-acid generator with high acid yield. The sulfonimide photo-acid generator has a structure as shown in a general formula (A) in the description. The acid generator has high sensitivity to active energy rays with the wavelength of 300-450nm, particularly 365nm (I rays) and 405nm (H rays), and is good in solubility and strong in acidity.