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Magnetic mesoporous silica nanoparticles as a theranostic approach for breast cancer: Loading and release of the poorly soluble drug exemestane.
Publication Type: Academic Journal
Source(s): International journal of pharmaceutics [Int J Pharm] 2022 May 10; Vol. 619, pp. 121711. Date of Electronic Publication: 2022 Apr 01.
Abstract: Exemestane has a limited aqueous solubility that leads to a very high variability in absorption when administrated orally. It is crucial to develop strategies to increase the solubility and bioavailability of this drug. To overcome these issues, the ai...
Large-scale synthesis of galeterone and lead next generation galeterone analog VNPP433-3β.
Publication Type: Academic Journal
Source(s): Steroids [Steroids] 2022 Sep; Vol. 185, pp. 109062. Date of Electronic Publication: 2022 Jun 08.
Abstract: VNPP433-3β (compound 2, (3β-(1H-imidazole-1-yl)-17-(1H-benzimidazole-1-yl)-androsta-5,16-diene), a multitarget anticancer agent has emerged as our lead next generation galeterone analogs (NGGA). Here, we describe a large multi-gram (92 g) scale synthes...
Exemestane encapsulated polymer-lipid hybrid nanoparticles for improved efficacy against breast cancer: optimization, in vitro characterization and cell culture studies.
Publication Type: Academic Journal
Source(s): Nanotechnology [Nanotechnology] 2021 Jul 20; Vol. 32 (41). Date of Electronic Publication: 2021 Jul 20.
Abstract: Polymer-lipid hybrid nanoparticles (PLHNPs) are novel nanoplatforms for the effective delivery of a lipophilic drug in the management of a variety of solid tumors. The present work was designed to develop exemestane (EXE) encapsulated D-alpha-tocophery...
Boronic-targeted albumin-shell oily-core nanocapsules for synergistic aromatase inhibitor/herbal breast cancer therapy.
Publication Type: Academic Journal
Source(s): Materials science & engineering. C, Materials for biological applications [Mater Sci Eng C Mater Biol Appl] 2019 Dec; Vol. 105, pp. 110099. Date of Electronic Publication: 2019 Aug 19.
Abstract: Multi-modality strategies of albumin-mediated drug accumulation in tumor, boronate-based active tumor targeting and synergistic cancer therapy were combined together for effective treatment of breast cancer. Herein we report the development of albumin-...
Intracellular Environment Improvement of Mycobacterium neoaurum for Enhancing Androst-1,4-Diene-3,17-Dione Production by Manipulating NADH and Reactive Oxygen Species Levels.
Publication Type: Academic Journal
Source(s): Molecules (Basel, Switzerland) [Molecules] 2019 Oct 25; Vol. 24 (21). Date of Electronic Publication: 2019 Oct 25.
Abstract: As one of the most significant steroid hormone precursors, androst-1,4-diene-3,17-dione (ADD) could be used to synthesize many valuable hormone drugs. The microbial transformation of sterols to ADD has received extensive attention in recent years. In a...
Comparative study of the binding mode between cytochrome P450 17A1 and prostate cancer drugs in the absence of haem iron.
Publication Type: Academic Journal
Source(s): Journal of biomolecular structure & dynamics [J Biomol Struct Dyn] 2019 Oct; Vol. 37 (16), pp. 4161-4170. Date of Electronic Publication: 2019 Jan 11.
Abstract: According to the X-ray crystal structures of CYP17A1 (including its complexes with inhibitors), it is shown that a hydrogen bond exists between CYP17A1 and its inhibitors (such as abiraterone and TOK-001). Previous short MD simulations (50 ns) suggeste...
E2112: Randomized Phase III Trial of Endocrine Therapy Plus Entinostat or Placebo in Hormone Receptor-Positive Advanced Breast Cancer. A Trial of the ECOG-ACRIN Cancer Research Group.
Publication Type: Academic Journal
Source(s): Journal of clinical oncology : official journal of the American Society of Clinical Oncology [J Clin Oncol] 2021 Oct 01; Vol. 39 (28), pp. 3171-3181. Date of Electronic Publication: 2021 Aug 06.
Abstract: Purpose: Endocrine therapy resistance in advanced breast cancer remains a significant clinical problem that may be overcome with the use of histone deacetylase inhibitors such as entinostat. The ENCORE301 phase II study reported improvement in progress...
Nanostructured Lipid Carriers for Oral Bioavailability Enhancement of Exemestane: Formulation Design, In Vitro, Ex Vivo, and In Vivo Studies.
Publication Type: Academic Journal
Source(s): Journal of pharmaceutical sciences [J Pharm Sci] 2019 Oct; Vol. 108 (10), pp. 3382-3395. Date of Electronic Publication: 2019 Jun 13.
Abstract: Exemestane (EXE) is a novel oral steroidal aromatase inhibitor approved for the treatment of breast cancer. However, its oral clinical application is limited because of low aqueous solubility and low oral bioavailability. Here, we aim to design and fab...
Phase 1 trial of entinostat as monotherapy and combined with exemestane in Japanese patients with hormone receptor-positive advanced breast cancer.
Publication Type: Academic Journal
Source(s): BMC cancer [BMC Cancer] 2021 Nov 24; Vol. 21 (1), pp. 1269. Date of Electronic Publication: 2021 Nov 24.
Abstract: Background: Entinostat is an oral inhibitor of class I histone deacetylases intended for endocrine therapy-resistant patients with hormone receptor-positive (HR+) advanced or metastatic breast cancer (BC). We examined the safety, efficacy, and pharmaco...
Discovery of novel 3-hydroxyandrosta-5,7-Diene-17-Carboxylic acid derivatives as anti-inflammatory bowel diseases (IBD) agents.
Publication Type: Academic Journal
Source(s): European journal of medicinal chemistry [Eur J Med Chem] 2021 Aug 05; Vol. 220, pp. 113468. Date of Electronic Publication: 2021 Apr 24.
Abstract: A series of steroidal compounds based on 3-hydroxyandrosta-5,7-diene-17-carboxylic acid core structure were designed, synthesized and bio-evaluated for their anti-inflammatory potency. Among them, compound 5c, 6f, and 6q effectively inhibited the produ...