Affiliation:
1. Department of Chemistry J.B. Institute of Engineering & Technology Yenkapally (V), Moinabad (M), Ranga Reddy (D), Hyderabad 500075 India
2. Department of Chemistry Chaitanya Deemed to be University Himayathnagar, Moinabad, Hyderabad, Telangana 500075 India
3. Department of Pharmacological Sciences Icahn School of Medicine at Mount Sinai Icahn Building, Room 16–50 A, 1425 Madison Aven, Manhattan New York NK-10029 USA
Abstract
AbstractIn this paper, we describe the synthesis of indolyl aryl sulfonamide conjugates (6 a–n). The anti‐tumour activity was assessed on three human cancer cell lines: A‐549 (lung), HeLa (cervix), and MCF‐7 (breast). Nocodazole was used as a standard drug by employing the MTT assay method. The results show that the compounds 6 b, 6 l, and 6 m have shown more potent activity as compared to the standard drug Nocodazole. In a cell survivability test (MCF‐10 A), three potent compounds (6 b, 6 l, and 6 m) were evaluated against the normal breast cell line, although neither of them displayed any significant cytotoxicity with IC50 values greater than 78.45 μM. Furthermore, the compounds 6 b, 6 l, and 6 m were tested for tyrosine kinase EGFR inhibitory action using Combretastatin A‐4 as the reference drug. The in vitro tubulin polymerization inhibitory activity indicates that the compounds 6b and 6 l showed promising potency with IC50 values of 2.40±0.02 and 2.34±0.03 mM, respectively. In addition to this, molecular docking studies of compounds 6 b, 6 l, and 6 m demonstrated that these compounds had more EGFR binding interactions. The potent compounds 6 b, 6 l, and 6 m were subjected to in silico pharmacokinetic assessment by SWISS, ADME, and pkCSM. While the compounds 6 b, 6 l, and 6 m followed five filters (Lipinski rule, Ghose rule, Veber rule, Egan rule, and Muegge rule) without any deviation.