Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives

Othman, Dina I. A.; Selim, Khalid B.; El‐Sayed, Magda A.‐A.; Tantawy, A.; Amen, Yhiya; Shimizu, Kuniyoshi; Okauchi, Tatsuo; Kitamura, Masaya

doi:10.1016/j.bmc.2019.07.042

Cited by 48 publications

(21 citation statements)

References 49 publications

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“…It consists of four distinct phases: the G1 phase, S phase (synthesis), G2 phase, and M phase 23,24,[50][51][52] . Apoptosis, that is, programmed cell death, is considered an important target of the most anti-tumour agents, resulting in G2/M arrest 23,24,[50][51][52] . Our promising derivatives 3 and 11 were subjected to cell cycle analysis and an apoptotic assay to investigate their roles in the cell cycle progression of HCT-116 and MCF-7 cells, respectively.…”

Section: Cell Cycle Arrest Analysis and Detection Of Apoptosismentioning

confidence: 99%

Design, synthesis, and analysis of antiproliferative and apoptosis-inducing activities of nitrile derivatives containing a benzofuran scaffold: EGFR inhibition assay and molecular modelling study

Fares

Selim

Goda

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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New cyanobenzofurans derivatives 2-12 were synthesised, and their antiproliferative activity was examined compared to doxorubicin and Afatinib (IC 50 ¼ 4.17-8.87 and 5.5-11.2 mM, respectively). Compounds 2 and 8 exhibited broad-spectrum activity against HePG2 (IC 50 ¼ 16.08-23.67 mM), HCT-116 (IC 50 ¼ 8.81-13.85 mM), and MCF-7 (IC 50 ¼ 8.36-17.28 mM) cell lines. Compounds 2, 3, 8, 10, and 11 were tested as EGFR-TK inhibitors to demonstrate their possible anti-tumour mechanism compared to gefitinib (IC 50 5 0.90 mM). Compounds 2, 3, 10, and 11 displayed significant EGFR TK inhibitory activity with IC 50 of 0.81-1.12 mM. Compounds 3 and 11 induced apoptosis at the Pre-G phase and cell cycle arrest at the G2/ M phase. They also increased the level of caspase-3 by 5.7-and 7.3-fold, respectively. The molecular docking analysis of compounds 2, 3, 10, and 11 indicated that they could bind to the active site of EGFR TK.

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Section: Cell Cycle Arrest Analysis and Detection Of Apoptosismentioning

confidence: 99%

Design, synthesis, and analysis of antiproliferative and apoptosis-inducing activities of nitrile derivatives containing a benzofuran scaffold: EGFR inhibition assay and molecular modelling study

Fares

Selim

Goda

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Compound 96 (IC 50 = 17.5 μM), 98 d (IC 50 = 38.4 μM) and 98 e (IC 50 = 28.3 μM) exhibited most potent anticancer activity against HeLa and MCF7 as compared to standard 5-FU by the inhibition of Topo II and EGFR-TK enzymes, implying its significance for further exploration (Scheme 20). [82]…”

Section: Quinoline-thiophene Hybridsmentioning

confidence: 99%

Navigating the Synthesis of Quinoline Hybrid Molecules as Promising Anticancer Agents

Panda

Chakroborty

2020

ChemistrySelect

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The emergence of drug resistance and low specificity with side effects are the significant challenges in pharmaceutical sectors for control of cancer nowadays. Notwithstanding, this is an imperative prerequisite to develop novel anticancer agents through mainstream medicinal chemistry approaches. The intriguing quinoline and its derivatives have demonstrated as significant building blocks for the locating of new promising anticancer agents. Consequently, quinoline moiety with the addition of suitable congeners would offer a strategy for the development of potential drug candidates. This present review article summarizes the recent advances (2018‐2020) of quinoline hybrids and their anticancer activity. The mechanism action and plausible structure‐activity relationship have discussed.

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“…A 2-chloroquinoline-thiophene scaffod was modified at its 3-position with oxazole/triazole/benzyl derivatives to produce a set of quinoline derivatives. [99] Growth inhibitory properties of the designed derivatives were explored against proliferation of . Sulfur and Silicon containing anticancer quinoline molecules B.…”

Section: Phosphorous Silicon and Sulfur-containing Quinoline Analogsmentioning

confidence: 99%

“…Sulfur and Silicon containing anticancer quinoline molecules B. [95][96][97][98][99] potent MCF-7 inhibitory properties with IC 50 values of 38.…”

Section: Phosphorous Silicon and Sulfur-containing Quinoline Analogsmentioning

confidence: 99%

Report on Recently (2017–20) Designed Quinoline‐Based Human Cancer Cell Growth Inhibitors

Dorababu¹

2020

ChemistrySelect

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Quinoline has been a most essential pharmacophore, derivatization of which led to enticing pharmacological properties. Quinoline is responsible for a wide range of biological potencies such as antibacterial, antifungal, anti-leishmanial, antimalarial, antioxidant and anticancer properties. Out of these clinical importances, the anticancer property of heterocycles is of greatest concern as cancer has become a major threat globally. Since some natural products containing quinoline moiety have displayed cancer inhibition potency, quinoline has been given highest priority in the anticancer drug design and development. In addition, quinoline has got eight positions including nitrogen for substitution which may result in some potential anticancer properties. Ever since, this extraordinary potential is being utilized in anticancer drug discovery. In this review, the various trends in drug design of quinoline moiety anticipating finest anticancer properties through cancer cell growth inhibition are collated comprehensively. The review work is classified based on type of quinoline derivatives. Besides this, with the aid of structure-activity relationship discussion, the importance of structural units that contributed to strongest activity towards cancer inhibition is emphasized. The particular activity would help to bring further advanced anticancer agents in the future.

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Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives

Cited by 48 publications

References 49 publications

Design, synthesis, and analysis of antiproliferative and apoptosis-inducing activities of nitrile derivatives containing a benzofuran scaffold: EGFR inhibition assay and molecular modelling study

Design, synthesis, and analysis of antiproliferative and apoptosis-inducing activities of nitrile derivatives containing a benzofuran scaffold: EGFR inhibition assay and molecular modelling study

Navigating the Synthesis of Quinoline Hybrid Molecules as Promising Anticancer Agents

Report on Recently (2017–20) Designed Quinoline‐Based Human Cancer Cell Growth Inhibitors

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