Sigalapalli, DK; Pooladanda, V; Kadagathur, M; Guggilapu, SD; Uppu, JL; Godugu, C; Bathini, NB; Tangellamudi, ND in [Sigalapalli, Dilep Kumar; Kadagathur, Manasa; Guggilapu, Sravanthi Devi; Uppu, Jaya Lakshmi; Tangellamudi, Neelima D.] Natl Inst Pharmaceut Educ & Res NIPER, Dept Med Chem, Hyderabad 500037, Andhra Pradesh, India; [Bathini, Nagendra Babu] Indian Inst Chem Technol, CSIR, Fluoroagrochem, Hyderabad 500007, Andhra Pradesh, India; [Pooladanda, Venkatesh; Godugu, Chandraiah] Natl Inst Pharmaceut Educ & Res NIPER, Dept Regulatory Toxicol, Hyderabad 500037, Andhra Pradesh, India; [Guggilapu, Sravanthi Devi] NIDDK, NIH, Lab Bioorgan Chem, Bethesda, MD 20892 USA published Novel chromenyl-based 2-iminothiazolidin-4-one derivatives as tubulin polymerization inhibitors: Design, synthesis, biological evaluation and molecular modelling studies in 2021.0, Cited 52.0. Recommanded Product: 3,4-Dimethoxybenzaldehyde. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9.
Here-in, we present molecular design, chemical synthesis and evaluation of novel chromenyl-based 2-iminothiazolidin-4-one derivatives as tubulin polymerization inhibitors. The newly synthesized compounds were evaluated for their in vitro cytotoxicities against A549 (lung cancer), MDA-MB-231 and BT-471 (breast cancer), HepG2 (liver cancer) and HCT-116 (colon cancer) cell lines by MTT assay. Among the synthesized compounds, compound 12b showed excellent anticancer activity on MDA-MB-231 cell line with IC50 value of 0.95 +/- 1.88 mu M and was verified to be safe in normal human bronchial epithelial cells (Beas-2B). Apoptosis induced by the lead 12b was observed using morphological observations, AO/EB and DAPI staining procedures. Further, dose-dependent increase in the depolarization of mitochondrial membrane was also observed through JC-1 staining. Annexin V-FITC/PI assay confirmed that 12b induced early apoptosis. Additionally, cell cycle analysis indicated that the MDA-MB-231 cells were arrested at sub-G2/M phase and also inhibited tubulin polymerization with IC50 value of 3.54 +/- 0.2 mM. Molecular docking simulations were employed to identify the important binding modes responsible for the tubulin inhibitory activity, thus supporting their effective anticancer potential. (c) 2020 Published by Elsevier B.V.
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,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles