Novel Coumarin‐steroid/terpenoid Hybrids: In vitro and in silico Anticancer Studies DOI Open Access

Rosa I. Martínez-Lara,

Luis A. Cobos-Ontiveros,

Silvia Alejandra Meza-Ireta

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: unknown

Published: Aug. 13, 2024

Abstract We have synthesized a series of novel coumarin‐steroid and triterpenoid hybrids evaluated their potential anticancer activity through molecular docking calculations in vitro antiproliferative assays. These hybrids, derived from estrone oleanolic acid, were linked via hydrocarbon spacers varying lengths. Molecular studies against human aromatase revealed strong interactions, particularly for compound 11d , which exhibited significant binding affinity (−12.6308 kcal/mol). In assays demonstrated that compounds 6b had notable effects, with GI 50 values 5.4 7.0 μM WiDr (colon) HeLa (cervix) cancer cells, respectively. findings highlight the these as agents targeting aromatase, warranting further investigation optimization.

Language: Английский

Aromatase Inhibitors as a Promising Direction for the Search for New Anticancer Drugs DOI Creative Commons
Sara Janowska, Serhii Holota, Roman Lesyk

et al.

Molecules, Journal Year: 2024, Volume and Issue: 29(2), P. 346 - 346

Published: Jan. 10, 2024

Aromatase is an enzyme that plays a crucial role in the biosynthesis of estrogens, which are hormones contribute to growth certain types breast cancer. In particular, aromatase catalyzes conversion androgens (male hormones) into estrogens (female various tissues, including adrenal glands, ovaries, and adipose tissue. Given estrogen promoting hormone-receptor-positive cancers, has become important molecular target for development anticancer agents. inhibitors can be classified two main groups based on their chemical structure: steroidal non-steroidal inhibitors. This work presents review literature from last ten years regarding search new We present directions search, taking account impact structure modifications activity.

Language: Английский

Citations

9
Discovery and development of steroidal enzyme inhibitors as anti-cancer drugs: state-of-the-art and future perspectives DOI Creative Commons
Bruno Cerra, Antimo Gioiello

Journal of Enzyme Inhibition and Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 40(1)

Published: April 2, 2025

Steroidal compounds have emerged as effective therapeutic agents in oncology. Beyond natural-occurring and synthetic steroids that act cytotoxic anti-tumoral agents, steroidal derivatives can be designed to mime the endogenous substrates of key metabolic enzymes steroidogenesis, thus reducing circulating levels relevant oestrogenic androgenic hormones responsible for cancer survival proliferation. Therefore, enzyme inhibition represents an intriguing endocrine approach treatment hormone-dependent tumours, such breast prostate cancer, with well-known approved drugs several pre-clinical clinical candidates under investigation. This review summarises advancements over past decade (2014-2024) development inhibitors endowed anticancer activity, illustrating their mechanisms action, potential, drug design approaches, current applications. Furthermore, we discuss challenges related resistance, off-target effects, future strategies optimise efficacy

Language: Английский

Citations

0
Syntheses and medicinal chemistry of spiro heterocyclic steroids DOI Creative Commons
Laura L. Romero-Hernández, Ana I. Ahuja‐Casarín, Penélope Merino‐Montiel

et al.

Beilstein Journal of Organic Chemistry, Journal Year: 2024, Volume and Issue: 20, P. 1713 - 1745

Published: July 24, 2024

There is compelling evidence that incorporating a heterocyclic moiety into steroid can alter its pharmacological and pharmacokinetic properties, driving intense interest in the synthesis of such hybrids among research groups. In this review, we present an overview recent synthetic methodologies, spanning period from 2000 to 2023, for preparation spiro steroids. The compounds surveyed encompass four-, five-, six-, seven-membered heterocycles appended various positions steroidal backbones, with spirocycles containing oxygen, nitrogen, sulfur atoms being predominant. outlined procedures emphasize pivotal steps constructing heterocycles, often accompanied by detailed account overall pathway. review encompasses innovative compounds, including bis-steroids linked heterocycle steroids conjugated moieties three or more (hetero)cycles. Moreover, many are data on their biological activities, as antiproliferative, antimalarial, antimicrobial, antifungal, antagonist, enzyme inhibition, others, aimed at furnishing pertinent insights future design potent selective drugs.

Language: Английский

Citations

2
Novel Coumarin‐steroid/terpenoid Hybrids: In vitro and in silico Anticancer Studies DOI Open Access

Rosa I. Martínez-Lara,

Luis A. Cobos-Ontiveros,

Silvia Alejandra Meza-Ireta

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: unknown

Published: Aug. 13, 2024

Abstract We have synthesized a series of novel coumarin‐steroid and triterpenoid hybrids evaluated their potential anticancer activity through molecular docking calculations in vitro antiproliferative assays. These hybrids, derived from estrone oleanolic acid, were linked via hydrocarbon spacers varying lengths. Molecular studies against human aromatase revealed strong interactions, particularly for compound 11d , which exhibited significant binding affinity (−12.6308 kcal/mol). In assays demonstrated that compounds 6b had notable effects, with GI 50 values 5.4 7.0 μM WiDr (colon) HeLa (cervix) cancer cells, respectively. findings highlight the these as agents targeting aromatase, warranting further investigation optimization.

Language: Английский

Citations

1