Synthesis and biological evaluation of curcumin inspired imidazo[1,2-a]pyridine analogues as tubulin polymerization inhibitors

Ramya, P.V. Sri; Guntuku, Lalita; Angapelly, Srinivas; Digwal, Chander Singh; Lakshmi, Uppu Jaya; Sigalapalli, Dilep Kumar; Babu, Bathini Nagendra; Naidu, V.G.M.; Kamal, Ähmed

doi:10.1016/j.ejmech.2017.11.010

Cited by 47 publications

(48 citation statements)

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“…More recently, curcumin mimics bearing an additional bridged phenyl ring in conjugation [69], and a series of curcumin inspired imidazo [1,2-a]pyridine analogues [70] and indole analogues [71] have been synthesized. Several of these analogues efficiently blocked tubulin polymerization and exerted improved antiproliferative effects against various cancer cell lines.…”

Section: Structure-activity Relationshipsmentioning

confidence: 99%

Beyond the Paclitaxel and Vinca Alkaloids: Next Generation of Plant-Derived Microtubule-Targeting Agents with Potential Anticancer Activity

Zhang

Kanakkanthara

2020

Cancers

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Plants are an important source of chemically diverse natural products that target microtubules, one of the most successful targets in cancer therapy. Colchicine, paclitaxel, and vinca alkaloids are the earliest plant-derived microtubule-targeting agents (MTAs), and paclitaxel and vinca alkaloids are currently important drugs used in the treatment of cancer. Several additional plant-derived compounds that act on microtubules with improved anticancer activity are at varying stages of development. Here, we move beyond the well-discussed paclitaxel and vinca alkaloids to present other promising plant-derived MTAs with potential for development as anticancer agents. Various biological and biochemical aspects are discussed. We hope that the review will provide guidance for further exploration and identification of more effective, novel MTAs derived from plant sources.

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Section: Structure-activity Relationshipsmentioning

confidence: 99%

Beyond the Paclitaxel and Vinca Alkaloids: Next Generation of Plant-Derived Microtubule-Targeting Agents with Potential Anticancer Activity

Zhang

Kanakkanthara

2020

Cancers

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“…Dienone is an attractive chemical motif utilized by many researchers for designing promising biologically/ pharmacologically active agents. [1][2][3][4] Curcumin 1 is one of the most famous dietary natural product dienones isolated from Curcuma longa and used in many Asian countries for its anti-inammatory and wound healing properties (Ayurvedic medicine). [5][6][7] Curcumin analogues exhibit an extensive broad spectrum of biological properties such as antibacterial, 8 antitubercular, 9 anti-HIV, 10 antioxidant, 11 antitumor, 7 and anti-inammatory 12 activities and exhibit a potential therapeutic effect on Alzheimer's disease.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, human topoisomerase IIα inhibitory properties and molecular modeling studies of anti-proliferative curcumin mimics

et al. 2019

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“…Previous reports have demonstrated that the mitochondria play a crucial role in the intrinsic pathway of apoptosis since they are the pivotal targets of cellular oxidative stress, that impede with the electron transport chain, leading to reactive oxygen species (ROS) generation and collapse of ΔΨ M . Hence, we evaluated the impact of compound 10 w on mitochondria using JC‐1 staining . Treatment of MCF‐7 cells with 1, 2.5 and 5 μM of 10 w for 24 h resulted in the enhancement of depolarized cell population (P2) from 6.14% (control) to 9.15 (at 1 μM), 12.32% (at 2.5 μM) and 23.09% (at 5 μM), in concentration dependent manner (Figure ).…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Biological Evaluation of Thieno[2, 3‐d]pyrimidine‐amides as Potential Anticancer Agents

et al. 2018

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In our search towards the development of potential anticancer agents, a new class of N‐(3‐(thieno[2, 3‐d]pyrimidin‐4‐ylamino)phenyl)amides (10 a−x) were synthesized and examined for their anticancer activity towards different human cancer cell lines. Of the derivatives tested, 10 g, 10 p and 10 w displayed potent growth inhibition on some of the cell lines, peculiarly 10 w exhibited selective and promising activity on MDA‐MB‐453 and MCF‐7 cell lines. In comparison to the standard ZSTK474, nearly 3 fold growth inhibitory effect was noticed with 10 w against MCF‐7 cell line. Notably, the morphology and long term clonogenic survival of MCF‐7 cells were affected by compound 10 w. Moreover, the results from AO/EB and DAPI staining studies as well as analysis of mitochondrial membrane potential divulged that the growth of MCF‐7 cells was inhibited by 10 w through the induction of apoptosis. From flow‐cytometry analysis, it is notable that 10 w shows G0/G1 cell cycle arrest in MCF‐7 cells. Overall, compound 10 w could be considered as a promising lead for the further exploration and identification of thieno[2, 3‐d]pyrimidine‐based anticancer agents.

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Synthesis and biological evaluation of curcumin inspired imidazo[1,2-a]pyridine analogues as tubulin polymerization inhibitors

Cited by 47 publications

References 54 publications

Beyond the Paclitaxel and Vinca Alkaloids: Next Generation of Plant-Derived Microtubule-Targeting Agents with Potential Anticancer Activity

Beyond the Paclitaxel and Vinca Alkaloids: Next Generation of Plant-Derived Microtubule-Targeting Agents with Potential Anticancer Activity

Synthesis, human topoisomerase IIα inhibitory properties and molecular modeling studies of anti-proliferative curcumin mimics

Synthesis and Biological Evaluation of Thieno[2, 3‐d]pyrimidine‐amides as Potential Anticancer Agents

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