877-03-2Relevant articles and documents
Synthesis and photobiological applications of naphthalimide-benzothiazole conjugates: cytotoxicity and topoisomerase IIα inhibition
Choudhury, Diptiman,Luxami, Vijay,Paul, Kamaldeep,Singh, Iqubal
, p. 483 - 497 (2022/01/20)
Conjugates of naphthalimide, benzothiazole, and indole moieties are synthesized that show excellent cytotoxicity against A549 (lung), MCF7 (breast), and HeLa (cervix) cancer cell lines with IC50 values in the range of 0.14-8.59 μM. Compounds 12 and 13 substituted with ethanolamine and propargyl groups reveal potent cytotoxicity towards A549 cancer cells with IC50 values of 140 and 310 nM, respectively. These compounds are further evaluated as potent inhibitors of human type IIα topoisomerase. These conjugates also reveal strong interaction towards human serum albumin (HSA) with binding constant values of 1.75 × 105 M-1 and 1.88 × 105 M-1, respectively, and formation of the stable complex at ground state with static quenching. Docking studies also confirm the effective interactions between conjugates and topoisomerase. This journal is
Synthesis, Characterization, and Antioxidant Properties of Novel 1-(4-Aryl-1,3-thiazol-2-yl)-2-{[1-(3-methylbut-2-en-1-yl)-1H-indol-3-yl]methylidene}hydrazines
Durgeswari, L. K.,Ganta, Ravi Kumar,Murthy, Y. L. N.
, p. 1552 - 1558 (2021/10/26)
Abstract: A series of novel 1-(4-aryl-1,3-thiazol-2-yl)-2-{[1-(3-methylbut-2-en-1-yl)-1H-indol-3-yl]methyli-dene}hydrazines were synthesized and properly characterized through IR, 1H and 13C NMR, and HRMS spectroscopic techniques. The synthesized compounds were screened for their antioxidant properties by using DPPH radical scavenging assay in comparison to ascorbic acid used as standard. The presence of a prenyl chain makes those compounds more lipophilic, which plays a crucial role in their radical scavenging activity. 1-{5-Bromo-[1-(3-methylbut-2-enyl)-1H-indole-3-yl]methylidene}-2-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hy-dra-zine showed a promising antioxidant activity.
Design, synthesis, anticancer activity, molecular docking and ADME studies of novel methylsulfonyl indole-benzimidazoles in comparison with ethylsulfonyl counterparts
Karadayi, Fikriye Zengin,Yaman, Murat,Kisla, Mehmet Murat,Konu, Ozlen,Ates-Alagoz, Zeynep
, p. 9010 - 9019 (2021/06/06)
Cancer poses a world-wide healthcare problem, demanding selective and effective therapy protocols. To address that, a vast amount of therapeutic candidates are being investigated in the field of medicinal chemistry. Accordingly, indole-benzimidazole structures have recently gained considerable interest because of their anticancer properties and estrogen receptor (ER) modulatory actions. In this study, novel methylsulfonyl indole-benzimidazole derivatives have been synthesized upon substitution of respectively the first (R1) and fifth (R2) positions of benzimidazole and indole groups. Structure and activity relationships were then studied via1H NMR, 13C NMR, mass spectral and in silico docking analyses, as well as cell viability measurements. We found that the compounds exhibited substantial affinity levels towards ER alpha (ERα). In addition, the correlation analysis of cytotoxicity profiles between ethyl- and methyl-sulfonyl indole-benzimidazoles revealed a collection of effective and consistent R1 and R2 substitutions. However, for some candidate derivatives, distinctive cytotoxicity levels and varying viability versus ERα affinity correlations were observable across the studies, suggesting that the sulfonyl side chain modifications themselves can also influence the ERα binding levels. These results demonstrated that our novel methylsulfonyl indole-benzimidazole derivatives, similar to their ethylsulfonyl counterparts, exhibit anticancer effects with potential estrogen receptor modulatory actions. This journal is
