Design, synthesis and biological evaluation of novel estrogen-derived steroid metal complexes

Zhang, Xinlong; Zuo, Ziqing; Tang, Juan; Wang, Kai; Wang, Caihua; Li, Changhao; Xu, W.; Xiong, Xiaolin; Yuntai, Kangxiang; Huang, Jian; Lan, Xiaoli; Zhou, Hai-Bing

doi:10.1016/j.bmcl.2013.04.088

Cited by 17 publications

(16 citation statements)

References 42 publications

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“…Results showed that all of the compounds in this series were agonists on ERα. Compared to the neutral free ligand ( 45 , Figure 17 ), the binding affinity of compound 46a – c for ERα increased, while the binding affinity of 46a – c for ERβ all decreased [ 93 ].…”

Section: Metal Complexesmentioning

confidence: 99%

Estrogen Receptor Ligands: A Review (2013–2015)

Farzaneh

Zarghi

2016

Sci. Pharm.

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Estrogen receptors (ERs) are a group of compounds named for their importance in both menstrual and estrous reproductive cycles. They are involved in the regulation of various processes ranging from tissue growth maintenance to reproduction. Their action is mediated through ER nuclear receptors. Two subtypes of the estrogen receptor, ERα and ERβ, exist and exhibit distinct cellular and tissue distribution patterns. In humans, both receptor subtypes are expressed in many cells and tissues, and they control key physiological functions in various organ systems. Estrogens attract great attention due to their wide applications in female reproductive functions and treatment of some estrogen-dependent cancers and osteoporosis. This paper provides a general review of ER ligands published in international journals patented between 2013 and 2015. The broad physiological profile of estrogens has attracted the attention of many researchers to develop new estrogen ligands as therapeutic molecules for various clinical purposes. After the discovery of the ERβ receptor, subtype-selective ligands could be used to elicit beneficial estrogen-like activities and reduce adverse side effects, based on the different distributions and relative levels of the two ER subtypes in different estrogen target tissues. Therefore, recent literature has focused on selective estrogen ligands as highly promising agents for the treatment of some types of cancer, as well as for cardiovascular, inflammatory, and neurodegenerative diseases. Estrogen receptors are nuclear transcription factors that are involved in the regulation of many complex physiological functions in humans. Selective estrogen ligands are highly promising targets for treatment of some types of cancer, as well as for cardiovascular, inflammatory and neurodegenerative diseases. Extensive structure-activity relationship studies of ER ligands based on small molecules indicate that many different structural scaffolds may provide high-affinity compounds, provided that some basic structural requirements are present.

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Section: Metal Complexesmentioning

confidence: 99%

Estrogen Receptor Ligands: A Review (2013–2015)

Farzaneh

Zarghi

2016

Sci. Pharm.

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“…Substituents with different stereoelectronic properties and Substantial inhibition can be seen for compounds 15-20 all of them sharing a cinchona-based substituent. Interestingly, the presence of a 3,5-bisĲtrifluoromethyl)phenyl moiety confers almost in all the cases inhibition of cell viability (15,16,21,27,(34)(35)(36)(37)(38), irrespective of the other substituent present at the second amide. Similarly, 3,5-bisĲtrifluoromethyl)benzyl substituted squaramides 22 and 26 also show good activities in HGC-27 cells, whereas they are less active in HeLa cells.…”

Section: Resultsmentioning

confidence: 98%

“…7 This has promoted recent interest of medicinal chemists in considering squaramide motifs as promising candidates for drug design and interesting tools as bioisosteres of ureas, guanidines or phosphates, among others. [8][9][10][11][12][13][14][15][16] Moreover, squaramides exhibit an interesting dual behaviour, as they are able to act as good hydrogen bond acceptors and hydrogen bond donors, which make them suitable for both cation and anion recognition. This could be crucial for the success of cell internalization of these compounds, one of the most important issues in drug design.…”

Section: Introductionmentioning

confidence: 99%

Squaramides with cytotoxic activity against human gastric carcinoma cells HGC-27: synthesis and mechanism of action

et al. 2016

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“…В работах других исследователей синтезированы конъюгаты тестостерона, содержащие комплексы Re (V) и радиоактивного 99 Tc, а также конъюгаты эстра диола, содержащие комплексы Pd, Ni и Zn 62-68 (рис. 7) [67][68][69].…”

Section: конъюгаты стероидов с лекарственными препаратамиunclassified

“…Он может быть использован в качестве метки для радиодиагностики и радиотерапии [68]. Конъюгаты 66-68 обладали определенным сродством к эстрогеновому рецептору (≈2 % связывания эстрадиола) и проявляли свойства агонистов этого рецептора [69]. 16 [83].…”

Section: конъюгаты стероидов с лекарственными препаратамиunclassified

Steroid Conjugates as Potential Anti-Cancer Agents

Zolottsev

Latysheva

Покровский

et al. 2020

Rossijskij bioterapevtičeskij žurnal

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The review is dedicated to results of investigations of steroid conjugates published predominantly over the past decade. It consists of three parts in which the data concerning biological activity of steroid conjugates with known drugs, steroid dimers, and steroid conjugates with some natural compounds, their fragments and related derivatives and analogs, are discussed. The structures of 231 steroid conjugates and their anti-cancer properties are presented.

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Design, synthesis and biological evaluation of novel estrogen-derived steroid metal complexes

Cited by 17 publications

References 42 publications

Estrogen Receptor Ligands: A Review (2013–2015)

Estrogen Receptor Ligands: A Review (2013–2015)

Squaramides with cytotoxic activity against human gastric carcinoma cells HGC-27: synthesis and mechanism of action

Steroid Conjugates as Potential Anti-Cancer Agents

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