Steroid Conjugates as Potential Anti-Cancer Agents

Zolottsev, Vladimir A.; Latysheva, Alexandra S.; Покровский, В. С.; Khan, Irina I.; Алманза, Р.Л. М.; Мишарин, А. Ю.

doi:10.17650/1726-9784-2019-19-1-22-52

Cited by 2 publications

(1 citation statement)

References 107 publications

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“…Recently, several reviews highlighting the varied therapeutic significance of steroid–amino acid conjugates and bile acid–bioactive molecule conjugates have been published. The therapeutic use of steroidal bioconjugates in cancer therapy has also been widely explored as indicated by numerous relevant literature reports. − In light of this, we thought it worthwhile to present a comprehensive review on the structurally diverse steroidal bioconjugates of potential therapeutic interest. This review covers the potential biological applications of steroidal bioconjugates and would benefit the wider scientific community in their drug discovery endeavors.…”

Section: Steroidal Bioconjugatesmentioning

confidence: 99%

A Comprehensive Review on Steroidal Bioconjugates as Promising Leads in Drug Discovery

Bansal

Suryan

2022

ACS Bio Med Chem Au

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Ever increasing unmet medical requirements of the human race and the continuous fight for survival against variety of diseases give birth to novel molecules through research. As diseases evolve, different strategies are employed to counter the new challenges and to discover safer, more effective, and target-specific therapeutic agents. Among several novel approaches, bioconjugation, in which two chemical moieties are joined together to achieve noticeable results, has emerged as a simple and convenient technique for a medicinal chemist to obtain potent molecules. The steroid system has been extensively used as a privileged scaffold gifted with significantly diversified medicinal properties in the drug discovery and development process. Steroidal molecules are preferred for their rigidness and good ability to penetrate biological membranes. Slight alteration in the basic ring structure results in the formation of steroidal derivatives with a wide range of therapeutic activities. Steroids are not only active as such, conjugating them with various biologically active moieties results in increased lipophilicity, stability, and target specificity with decreased adverse effects. Thus, the steroid nucleus prominently behaves as a biological carrier for small molecules. The steroid bioconjugates offer several advantages such as synergistic activity with fewer side effects due to reduced dose and selective therapy. The steroidal bioconjugates have been widely explored for their usefulness against various disorders and have shown significant utility as anticancer, anti-inflammatory, anticoagulant, antimicrobial, insecticidal/pesticidal, antioxidant, and antiviral agents along with several other miscellaneous activities. This work provides a comprehensive review on the therapeutic progression of steroidal bioconjugates as medicinally active molecules. The review covers potential biological applications of steroidal bioconjugates and would benefit the wider scientific community in their drug discovery endeavors.

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Section: Steroidal Bioconjugatesmentioning

confidence: 99%

A Comprehensive Review on Steroidal Bioconjugates as Promising Leads in Drug Discovery

Bansal

Suryan

2022

ACS Bio Med Chem Au

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Antiproliferative activity of the novel CYP17A1 inhibitor alsevirone

Khan,

Latysheva,

Zolottsev

et al. 2023

Russian Journal of Oncology

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BACKGROUND: Prostate cancer is the most frequently diagnosed type of cancer in men in developed countries. It is dependent upon androgens and could be effectively combated by androgen deprivation therapy. Reduction of androgen synthesis can be accomplished through the inhibition of the enzyme 17α-hydroxylase/17.20-lyase (CYP17A1), which catalyzes two sequential reactions in the production of androgens. Steroid derivatives modified with nitrogen-containing heterocycles attract attention as antineoplastic agents for prostate cancer treatment due to their inhibitory potential against CYP17A1. AIM: Evaluate cytotoxic activity and antitumor effects of the synthesized alsevirone in comparison with abiraterone. METHODS: Cytotoxicity was evaluated using MTT test. Anticancer effect was researched in vivo in prostate cancer xenograft models 22Rv1 and DU145 in Balb/c nude mice. Testosterone concentration was determined using an enzyme-linked immunosorbent assay in blood serum of BDF1 mice. RESULTS: Alsevirone demonstrated cytotoxic activity in prostate cancer cells: DU145 (23.8±1.2 µM vs 151.4±23.7 µM for abiraterone), 22Rv1 (35.9±5.6 µM vs 109.9±35.2 µM for abiraterone) and LNCaP (22.9±0.5 µM vs 28.8±1.6 µM for abiraterone). Testosterone concentration in blood serum of BDF1 mice reduced by 80% after 10-day treatment. Inhibition of the tumors’ growth in 22Rv1 xenograft model was statistically significant when using alsevirone in comparison with the control group: average tumor volume was 171.6±50.1 mm3 (р=0.022) vs 424.2±70.3 mm3 in control, with tumor growth inhibition index of 59%. CONCLUSIONS: Alsevirone has a higher cytotoxic potential against prostate cancer cells (DU145, LNCaP and 22Rv1) compared to abiraterone. Alsevirone demonstrated the ability to reduce the concentration of testosterone in the blood serum of BDF1 mice, and statistically significant antitumor activity in 22Rv1 xenograft models.

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Steroid Conjugates as Potential Anti-Cancer Agents

Cited by 2 publications

References 107 publications

A Comprehensive Review on Steroidal Bioconjugates as Promising Leads in Drug Discovery

A Comprehensive Review on Steroidal Bioconjugates as Promising Leads in Drug Discovery

Antiproliferative activity of the novel CYP17A1 inhibitor alsevirone

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