Synthesis and preliminary evaluation steroidal antiestrogen–geldanamycin conjugates

Hendricks, J. Adam; Hanson, Robert N.; Amolins, Michael W.; Mihelcic, John; Blagg, Brian S. J.

doi:10.1016/j.bmcl.2013.03.116

Cited by 6 publications

(2 citation statements)

References 25 publications

(29 reference statements)

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“…These findings established further investigations by the research group, focusing on molecules containing an antiestrogenic element connected to a traditional antitumor agent, like doxorubicin [98], mitomycin C [99] or geldanamycin [100], via a linker at position C11β. In fact, these compounds can be considered as conjugates or hybrid molecules.…”

Section: Antiestrogensmentioning

confidence: 67%

Steroidal Anticancer Agents: An Overview of Estradiol-related Compounds

Minorics

Zupkó

2018

ACAMC

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Research of steroidal compounds as anticancer agents started almost 50 years ago. During the past decades, several innovative new steroids, like cyproterone, finasteride, estramustin, exemestane and fulvestrant have successfully become a part of routine clinical practice. Meanwhile, a vast amount of new information have accumulated about the functions of the endogenous steroid system (including the characterization of enzymes, receptors, transcription pathways, etc.) and about the role of steroids in carcinogenesis. Therefore, it is regularly required to review the latest published results, focusing on a well-defined part within this research field that has definitely developed into a highly diversified speciality by now. Herein, we make an attempt to summarize the most recent results reported about anticancer agents of estrane backbone, focusing on their mechanisms of action and their structure-activity relationships. Due to the vast number and various accessibilities of scientific publications, neither other reviews nor this one can be considered as absolutely exhaustive. In spite of these restrictive factors, the current review makes a good opportunity to define the recent scientific trends in the field of estradiol-related anticancer agents.

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Section: Antiestrogensmentioning

confidence: 67%

Steroidal Anticancer Agents: An Overview of Estradiol-related Compounds

Minorics

Zupkó

2018

ACAMC

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“…These 11β‐E2‐GDA hydrids have higher binding affinity for ER but were less cytotoxic to ER + cells compared to ER – cells than the free drug GDA. Longer spacer lengths such as that in 40 tended to increase the binding efficacies (RBA of 39% relative to AE RU39411) …”

Section: Examples Of Targeting Molecules and Their Small‐molecule Conmentioning

confidence: 99%

Small Molecules for Active Targeting in Cancer

Kue

Kamkaew

Burgess

et al. 2016

Medicinal Research Reviews

115

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For the purpose of this review, active targeting in cancer research encompasses strategies wherein a ligand for a cell surface receptor expressed on tumor cells is used to deliver a cytotoxic or imaging cargo. This area of research is more than two decades old, but in those 20 and more years, how many receptors have been studied extensively? What kinds of the ligands are used for active targeting? Are they mostly naturally occurring molecules such as folic acid, or synthetic substances developed in campaigns for medicinal chemistry efforts? This review outlines the most important receptor or ligand combinations that have been used in active targeting to answer these questions, and therefore to address the most important one of all: is research in active targeting affording diminishing returns, or is this an area for which the potential far exceeds progress made so far?

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