Synthesis and antineoplastic activity of 2-alkylaminoethyl derivatives of various steroidal oximes
Abstract
Various steroidal oxime ether derivatives in androstene and estrane series have been synthesized and evaluated for the antineoplastic activity at National Cancer Institute, Bethesda, Maryland, USA. O-alkylation of the oximes by various alkylaminoethyl halides gave the oxime ether derivatives. The 17alpha-ethynylandrostene derivatives 29 (DPJ-684), 30 (DPJ-685), 31 (DPJ-686) and estrane derivatives 35 (DPJ-531) and 36 (DPJ-532) were among the small percentage of compounds, which have been screened by NCI for in vivo hollow fiber assay by virtue of their activity against one or more human tumour cell lines in 60 cell line in vitro prescreen. The preliminary in vivo reports of hollow fiber assays have been referred to the Biological Evaluation Committee for Cancer Drugs for considering these compounds for further detailed in vivo testing.
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Certain steroidal oximes and oxime ethers have antineoplastic activity.
“Certain steroidal oximes and oxime ethers were shown to have antioxidant [1], antimicrobial [1], antineoplastic [2] or neuromuscular blocking [3] activities.”
From Nitrogen-containing ecdysteroid derivatives vs. multi-drug resistance in cancer: Preparation and antitumor activity of oximes, oxime ethers and a lactam (2018) · cites this paper as [2]
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- Authors
- Jindal, D. P., Chattopadhaya, R., Guleria, S., & Gupta, R.
- Affiliations
- Panjab University (IN)
- Corresponding author
- Gupta, Ranju
- ORCID
- Gupta, Ranju
- Venue
- European Journal of Medicinal Chemistry
- Publisher
- Elsevier BV
- Published
- 2003-11
- Volume
- 38
- Issue
- 11-12
- Pages
- 1025-1034
- ISSN
- 0223-5234 (ISSN-L)
- OpenAlex
- W1967693558
- Cited by
- 52
- References
- 22
- Citations by year
- 2025: 2 · 2023: 5 · 2021: 1 · 2020: 3 · 2019: 1 · 2018: 1 · 2017: 2 · 2016: 2 · 2015: 6 · 2014: 4 · 2013: 3 · 2012: 1
- FWCI
- 0.94
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Council of Scientific and Industrial Research, India
- National Cancer Institute
- Topics
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Steroid Chemistry and Biochemistry
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Phytochemical Studies and Bioactivities
- Keywords
- oxime ethers, anticancer activity, O-alkylation, estrane derivatives, hollow fiber assay, human cancer cell lines, anticancer drug candidates
- MeSH terms
- Antineoplastic Agents, Humans, Oximes, Antineoplastic Agents, Alkylating, Cell Line, Tumor
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