Aromatase Inhibitors

Samara, Nivin; Casper, Robert F.

doi:10.1007/978-3-319-45534-1_10

Cited by 3 publications

(1 citation statement)

References 93 publications

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“…In the last few years, different studies approved that aromatase inhibitors (letrozole) is a good, effective and safe treatment modality in infertility and ovulation induction in PCOS. Moreover, use of letrozole has been recommended for patients who ovulate with clomiphene but have a thin endometrium [13].…”

Section: Discussionmentioning

confidence: 99%

Letrozole versus Gonadotropins for Ovulation Induction in Clomiphene Citrate Resistance: A Randomized Controlled Study

S¹,

S²,

M³

2021

Annals Gynecol Obstet

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Background: Clomiphene citrate resistance (CCR) occur in 15 -40% in women with PCOS. Several studies have shown that letrozole is superior to CC regarding side effects, ovulation, and pregnancy rates. Letrozole or gonadotropins use for ovulation induction in CCR is not well established which is superior and most safe.Aims: To compare between letrozole and gonadotropin in induction of ovulation in clomiphene citrate resistant cases.

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Section: Discussionmentioning

confidence: 99%

Letrozole versus Gonadotropins for Ovulation Induction in Clomiphene Citrate Resistance: A Randomized Controlled Study

S¹,

S²,

M³

2021

Annals Gynecol Obstet

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Developing multitarget coumarin based anti-breast cancer agents: synthesis and molecular modeling study

Takla,

Bayoumi,

El-Messery

et al. 2023

Sci Rep

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A new series of 7-substituted coumarin scaffolds containing a methyl ester moiety at the C4-position were synthesized and tested for their in vitro anti-proliferative activity against MCF-7 and MDA-MB-231 breast cancer cell lines using Doxorubicin (DOX) as reference. Compounds 2 and 8 showed noticeable selectivity against MCF-7 with IC50 = 6.0 and 5.8 µM, respectively compared to DOX with IC50 = 5.6 µM. Compounds 10, 12, and 14 exhibited considerable selectivity against Estrogen Negative cells with IC50 = 2.3, 3.5, and 1.9 µM, respectively) compared to DOX with (IC50 = 7.3 µM). The most promising compounds were tested as epidermal growth factor receptor and aromatase (ARO) enzymes inhibitors using erlotinib and exemestane (EXM) as standards, respectively. Results proved that compound 8 elicited the highest inhibitory activity (94.73% of the potency of EXM), while compounds 10 and 12 displayed 97.67% and 81.92% of the potency of Erlotinib, respectively. Further investigation showed that the promising candidates 8, 10, and 12 caused cell cycle arrest at G0–G1 and S phases and induced apoptosis. The mechanistic pathway was confirmed by elevating caspases-9 and Bax/Bcl-2 ratio. A set of in silico methods was also performed including docking, bioavailability ADMET screening and QSAR study

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Semisynthetic Triazoles as an Approach in the Discovery of Novel Lead Compounds

Morais

Francisco

Heberth

et al. 2021

COC

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: Historically, the medicinal chemistry is concerned with the approach of organic chemistry to new drug synthesis. Considering the fruitful collections of new molecular entities, the dedicated efforts for medicinal chemistry are rewarding. Planning and search of new and applicable pharmacologic therapies involve the altruistic nature of the scientists. Since the 19th century, notoriously the application of isolated and characterized plant-derived compounds in modern drug discovery and in various stages of clinical development highlight its viability and significance. Natural products influence a broad range of biological processes, covering transcription, translation, and post-translational modification and being effective modulators of almost all basic cellular processes. The research of new chemical entities through “click chemistry” continuously opens up a map for the remarkable exploration of chemical space in towards leading natural products optimization by structure-activity relationship. Finally, here in this review, we expect to gather a broad knowledge involving triazolic natural products derivatives, synthetic routes, structures, and their biological activities.

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Aromatase Inhibitors

Cited by 3 publications

References 93 publications

Letrozole versus Gonadotropins for Ovulation Induction in Clomiphene Citrate Resistance: A Randomized Controlled Study

Letrozole versus Gonadotropins for Ovulation Induction in Clomiphene Citrate Resistance: A Randomized Controlled Study

Developing multitarget coumarin based anti-breast cancer agents: synthesis and molecular modeling study

Semisynthetic Triazoles as an Approach in the Discovery of Novel Lead Compounds

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