Comparative differential cytotoxicity of clinically used SERMs in human cancer lines of different origin and its predictive molecular docking studies of key target genes involved in cancer progression and treatment responses

Lakshmi, S.; A, Shanitha; Dv, Shiny; Bs, Rahul; Saikant, R.; Sharaf, Shehna; Sa, Abi; Gopimohan, Rajmohan

doi:10.1016/j.crphar.2021.100080

Cited by 3 publications

(1 citation statement)

References 97 publications

(92 reference statements)

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“…Finally, the cytotoxic activity coefficients of compounds 10 and 11 were close to very high, and 13 had a very high correlation with tamoxifen, which is a selective estrogen receptor modulator that inhibits growth and promotes apoptosis in estrogen-receptor-positive tumors. 16 It also exhibits ER-independent anticancer effects by disrupting the mitochondrial bioenergetic function and inducing cell apoptosis. 17 This allows us to accept this mechanism of action as the leading route underlying the cytotoxic activity of these oxazole derivatives.…”

Section: Resultsmentioning

confidence: 99%

Design, synthesis and evaluation of the anti-breast cancer activity of 1,3-oxazolo[4,5-d]pyrimidine and 1,3-oxazolo[5,4-d]pyrimidine derivatives

et al. 2023

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Section: Resultsmentioning

confidence: 99%

Design, synthesis and evaluation of the anti-breast cancer activity of 1,3-oxazolo[4,5-d]pyrimidine and 1,3-oxazolo[5,4-d]pyrimidine derivatives

et al. 2023

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Antitumor Activity of Antiestrogen-Cytostatics and Their Binding Affinity with Estrogen Receptors

Dublin,

Semeikin,

Fedotcheva

et al. 2024

Pharm Chem J

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Molecular Docking Study on Tamoxifen and Toremifene's Effects on the Breast Cancer Receptors

Sulliman,

Ibrahim,

Ibrahim

et al. 2024

Turkish Computational and Theoretical Chemistry

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Both toremifene (TOR) and tamoxifen (TAM), selective estrogen receptor modulators, are equally effective therapies for breast cancer (BrCa). In high-risk women, anti-estrogenic tamoxifen is frequently used for both (BrCa) treatment and prevention. Another anti-estrogen that is successful in the treatment of (BrCa) is toremifene. Anti-estrogens have emerged as one of the most widely utilized medicine classes among women because (BrCa) is the most frequent malignancy in this population. Consequently, we performed a docking study to assess the effects of tamoxifen and toremifene therapy on the (BrCa) receptor. Tamoxifen and toremifene's interactions with the (BrCa) receptor were examined by a computational study of the ligand's binding. These receptors are named (1jnx), (1n5o), (1oqa), (1t2u), (1t29), (4igk), (4jlu), and (4y2g). All the docking has been done by software named Molecular Operating Environment (MOE) which was used to evaluate the binding docking and docking score between the ligand (TAM or TOR) with the (BrCa) receptors.

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Comparative differential cytotoxicity of clinically used SERMs in human cancer lines of different origin and its predictive molecular docking studies of key target genes involved in cancer progression and treatment responses

Cited by 3 publications

References 97 publications

Design, synthesis and evaluation of the anti-breast cancer activity of 1,3-oxazolo[4,5-d]pyrimidine and 1,3-oxazolo[5,4-d]pyrimidine derivatives

Design, synthesis and evaluation of the anti-breast cancer activity of 1,3-oxazolo[4,5-d]pyrimidine and 1,3-oxazolo[5,4-d]pyrimidine derivatives

Antitumor Activity of Antiestrogen-Cytostatics and Their Binding Affinity with Estrogen Receptors

Molecular Docking Study on Tamoxifen and Toremifene's Effects on the Breast Cancer Receptors

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