Synthesis, antiproliferative and pro-apoptotic activity of 2-phenylindoles

Kelly, P.M.; Bright, Sandra A.; Fayne, Darren; Pollock, Jade K.; Zisterer, Daniela M.; Williams, David C.; Meegan, Mary J.

doi:10.1016/j.bmc.2016.06.050

Cited by 21 publications

(5 citation statements)

References 54 publications

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“…Kelley et al [27], prepared a library of selective estrogen receptor modulators based on the 2-arylindole scaffolds to selectively target the estrogen receptor in hormone positive breast cancers (MCF-7). Among the synthesized compounds, compounds 23 and 24 (Table 7, Fig.…”

Section: Introductionmentioning

confidence: 99%

Estrogen alpha receptor antagonists for the treatment of breast cancer: a review

Sharma

Kumar

2018

Chemistry Central Journal

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BackgroundCancer is at present one of the leading causes of death in the world. It accounts for 13% of deaths occurred worldwide and is continuously rising, with an estimated million of deaths up to 2030. Due to poor availability of prevention, diagnosis and treatment of breast cancer, the rate of mortality is at alarming level globally. In women, hormone-dependent estrogen receptor positive (ER+) breast cancer making up approximately 75% of all breast cancers. Hence, it has drawn the extensive attention of researchers towards the development of effective drugs for the treatment of hormone-dependent breast cancer. Estrogen, a female sex hormone has a vital role in the initiation and progression of breast malignancy. Therefore, estrogen receptor is the central target for the treatment of breast cancer.ConclusionIn this review, we have studied various classes of antiestrogens that have been designed and synthesized with selective binding for estrogen alpha receptor (ER). Since estrogen receptor α is mainly responsible for the breast cancer initiation and progression, therefore there is need of promising strategies for the design and synthesis of new therapeutic ligands which selectively bind to estrogen alpha receptor and inhibit estrogen dependent proliferative activity.

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Section: Introductionmentioning

confidence: 99%

Estrogen alpha receptor antagonists for the treatment of breast cancer: a review

Sharma

Kumar

2018

Chemistry Central Journal

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“…Indole based tubulin inhibitors e. g . 2‐phenylindole derivatives are attractive anti‐breast cancer agents as shown in Figure ,. These derivatives can overcome multi‐drug resistance in cancer by interacting into the colchicine binding site on tubulin .…”

Section: Figurementioning

confidence: 99%

First Report on 3‐(3‐oxoaryl) Indole Derivatives as Anticancer Agents: Microwave Assisted Synthesis, In Vitro Screening and Molecular Docking Studies

et al. 2019

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In this study ZrCl4 was identified as an efficient Lewis acid catalyst for the synthesis of 3‐(3‐oxoaryl) indole derivatives via microwave assisted Michael addition of 2‐phenylindole with chalcones under solvent‐free condition. The reaction proceeds smoothly with high efficiency under green reaction condition to afford a range of 3‐(3‐oxoaryl) indole derivatives exclusively within a short period of time in excellent yields. The synthesized compounds have shown promising in vitro anticancer activity against murine melanoma (B16F10) and human breast cancer (MCF7) cell lines. Molecular docking analysis showed that this type of indole derivatives may act as anticancer agents through the inhibition of tubulin polymerization.

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“…7 Second-generation SERMs, including raloxifene and lasofoxifene, developed to avoid the uterotrophic effects of tamoxifen, are also not devoid of side effects such as intensifying the risk of blood clots, deep vein thrombosis, instigating hot flashes, and pulmonary embolism. 8 During recent developments in SERMs, 2-phenylindole analogs bazedoxifene and pipendoxifene were moved to clinical evaluations. 9 Bazedoxifene, a third-generation indole-based SERM developed by substituting the benzothiophene core of raloxifene with indole, is in a phase II clinical trial for treating BC.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents

Kaur,

Verma,

Gangwar

et al. 2024

RSC Med. Chem.

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Synthesis, antiproliferative and pro-apoptotic activity of 2-phenylindoles

Cited by 21 publications

References 54 publications

Estrogen alpha receptor antagonists for the treatment of breast cancer: a review

Estrogen alpha receptor antagonists for the treatment of breast cancer: a review

First Report on 3‐(3‐oxoaryl) Indole Derivatives as Anticancer Agents: Microwave Assisted Synthesis, In Vitro Screening and Molecular Docking Studies

Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents

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