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Author(s): Dr. R Sundhararajan.1, J. Seraphine Joyce*2, R. Abdul Basith3, K. Kalaiyarasi.4, P. Manju5, R .Vishnu Maaliga.6, A.Zainab Shaheen7

Email(s): 1theresa_sera@yahoo.com

Address:

    Mohamed Sathak AJ College of Pharmacy, Sholinganallur, Chennai-600119

Published In:   Volume - 5,      Issue - 3,     Year - 2026

DOI: https://doi.org/10.71431/IJRPAS.2026.5302  

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ABSTRACT:
Selective Estrogen receptor modulators (SERMs) interact with Estrogen receptors as agonists or antagonists depending on the target tissue. Currently available SERMs are used to address issues associated with PCOS, treat and prevent breast cancer, osteoporosis, to treat ovulatory dysfunction in women, and for assisting in contraception. PCOS ( Poly Cystic Ovarian Syndrome) is associated with abnormal function of the female sex hormone Estrogen and Estrogen receptors (ERs). Estrogens mediate genomic effects through ERα and ERβ in target tissues. The G-protein-coupled estrogen receptor (GPER) has recently been described as mediating the non-genomic signaling of estrogen. Changes in estrogen receptor signaling pathways affect cellular activities, such as ovulation; cell cycle phase; and cell proliferation, migration, and invasion. Future use of SERMs may also include their use in a Tissue Selective Estrogen Complex (TSEC), a therapy that combines a SERM with estrogen(s), designed to deliver the efficacy of each component with improved overall tolerability for the treatment of postmenopausal women. This article focuses on the rationale, design considerations, and therapeutic potential of thiourea-based bioisosteric SERMs with synthetic feasibility as novel Estrogen Receptor Modulators for the management of PCOS.

Cite this article:
Dr. R Sundhararajan., J. Seraphine Joyce, R. Abdul Basith, K. Kalaiyarasi. , P. Manju, R .Vishnu Maaliga., A.Zainab Shaheen Synthesis of Thiourea Derivatives as Bioisosteric Structures of SERMs Pursuant to Virtual Screening. IJRPAS, March 2026; 5(3): 15-24.DOI: https://doi.org/https://doi.org/10.71431/IJRPAS.2026.5302


1.        Schlesselman JJ. Risk of endometrial cancer in relation to use of combined oral contraceptives. A practitioner’s guide to meta‑analysis. Hum Reprod 1997;2:1851‑63.

2.        Gambineri A, Patton L, Vaccina A, Cacciari M, Morselli‑Labate AM, Cavazza C, etal. Treatment with flutamide, metformin, and their combination added to a hypocaloric diet in overweight‑obese women with polycystic ovary syndrome:A randomized,12‑month, placebo‑controlled study. J Clin Endocrinol Metab 2006;91:3970‑80.

3.        Farquhar C, Brown J, Marjoribanks J. Laparoscopic ‹drilling› by diathermy or laser for ovulation induction in anovulatory polycystic ovary syndrome. Cochrane Database Syst Rev  2012;6:CD001122.

4.        Thessaloniki ESHRE/ASRM‑Sponsored PCOS Consensus Workshop Group.Consensus on infertility treatment related topolycystic ovary syndrome. Fertil Steril 2008;89:505‑22.

5.        Asch RH, Greenblatt RB. Update on the safety and efficacyof clomiphene citrate as a therapeutic agent. J Reprod Med 1976;17:175‑80.

6.        Park JC, Lim SY, Jang TK, Bae JG, Kim JI, Rhee JH. Endometrialhistology and predictable clinical factors for endometrial disease in women with polycystic ovary syndrome. Clin Exp Reprod Med 2011;38:42‑6.

7.        Ghazeeri G, Kutteh WH, Bryer‑Ash M, Haas D, Ke RW. Effect ofrosiglitazone on spontaneous and clomiphene citrate‑induced ovulation in women with polycystic ovary syndrome. Fertil Steril 2003;79:562‑6.

8.        Rouzi AA, Ardawi MS. A randomized controlled trial of the efficacy of rosiglitazone and clomiphene citrate versus metformin and clomiphene citrate in women with clomiphene citrate‑resistant polycystic ovary syndrome. Fertil Steril 2006;85:428‑35.

9.        Johnson SR. Menopause and hormone replacement therapy. Med Clin North Am.

       1998;82:297–320.

10.    Helvaci N, Yildiz BO. Oral contraceptives in polycystic ovary syndrome. Minerva Endocrinol. 2014;39(3):175–187.

11.    Zhao X, Jiang Y, Xi H, et  al. Exploration of the relation-ship between gut microbiota and polycystic ovary syndrome (PCOS): a review. Geburtshilfe Frauenheilkd. 2020;80(2):161–171. doi: 10.1055/a-1081-2036.

12.    Vrieze A, Van Nood E, Holleman F, et  al. Transfer of intestinal microbiota from lean donors increases insulin sensitivity in individuals with metabolic syndrome. Gastroenterology. 2012;143(4):913–916.e7. doi:10.1053/j.gastro.2012.06.031.

13.    Heshmati J, Farsi F, Yosaee S, et  al. The effects of pro-biotics or synbiotics supplementation in women with polycystic ovarian syndrome: a systematic review and meta-analysis of randomized clinical trials. Probiot Antimicrob Proteins. 2019;11(4):1236–1247. doi:10.1007/s12602-018-9493-9.

14.    Shamasbi SG, Ghanbari-Homayi S, Mirghafourvand M. The effect of probiotics, prebiotics, and synbiotics on hormonal and inflammatory indices in women with polycystic ovary syndrome: a systematic review and meta-analysis. Eur J Nutr. 2019;59(2):433–450. doi: 10.1007/s00394-019-02033-1.

15.    An Y, Sun Z, Zhang Y, et  al. The use of berberine for women with polycystic ovary syndrome undergoing IVF treatment. Clin Endocrinol. 2014;80(3):425–431.

16.    Bahmani F, Karamali M, Shakeri H, et  al. The effects of folate supplementation on inflammatory factors and biomarkers of oxidative stress in overweight and obese women with polycystic ovary syndrome: a randomized, double-blind, placebo controlled clinical trial. Clin Endocrinol. 2014;81(4):582–587. doi: 10.1111/cen.12451.

17.    Lim SS, Kakoly NS, Tan JWJ, et  al. Metabolic syndrome in polycystic ovary syndrome: a systematic review, meta-analysis and meta-regression. Obes Rev. 2019;20(2):339–352. doi: 10.1111/obr.12762.

18.    Lord JM, Flight IH, Norman RJ. Metformin in polycystic ovary syndrome: systematic review and meta‑analysis. BMJ 2003;327:951‑3.

19.    Kumar P, Khan K. Effects of metformin use in pregnant patients with polycystic ovary syndrome. J Hum Reprod Sci2012;5:166‑9.

20.    Archer DF. The gynecologic effects of lasofoxifene, an estrogen agonist/antagonist, in postmenopausal women. Menopause.2011;18:67.doi:10.1097/gme.0b013e318203a46b.

 

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