Towards breast cancer targeting: Synthesis of tetrahydroindolocarbazoles, antibreast cancer evaluation, uPA inhibition, molecular genetic and molecular modelling studies

Ahmed, Entesar M.; Sarhan, Alaadin E.; Elnaggar, Dina H.; Khattab, Reham R.; El‐Naggar, Mohamed; El‐Messery, Shahenda M.; Hassan, Ghada S.; Mounier, Marwa M.; Mahmoud, Khaled; Ali, Nasar; Mahrous, Karima F.; Ali, Mamdouh M.; Sayed, Mardia T. El

doi:10.1016/j.bioorg.2019.103332

Cited by 8 publications

(3 citation statements)

References 33 publications

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“…Tetrahydroindolocarbazoles are further promising structural analogs of DIM, and compound 12 showed activity against MCF-7 breast cancer cells (IC 50 = 5.7 µmol/L). 12 inhibited the tumor-promoting factor uPA (urokinase plasminogen activator) which is overexpressed in various cancers including breast cancer [ 65 ] .…”

Section: Synthetic Dim Derivatives and Cancer Drug Resistancementioning

confidence: 99%

3,3’-Diindolylmethane and its derivatives: nature-inspired strategies tackling drug resistant tumors by regulation of signal transduction, transcription factors and microRNAs

Biersack¹

2020

CDR

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Indoles of cruciferous vegetables are promising anti-tumor agents. Studies with indole-3-carbinol and its dimeric product, 3,3'-diindolylmethane (DIM), suggest that these compounds have the ability to deregulate multiple cellular signaling pathways that are essential for tumor growth and spread. These natural compounds are also effective modulators of transcription factors and non-coding RNAs. These effects explain their ability to inhibit tumor spread and to overcome drug resistance. In this work, pertinent literature on the effects of DIM and its synthetic derivatives on resistant tumors and resistance mechanisms in tumors is highlighted.

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Section: Synthetic Dim Derivatives and Cancer Drug Resistancementioning

confidence: 99%

3,3’-Diindolylmethane and its derivatives: nature-inspired strategies tackling drug resistant tumors by regulation of signal transduction, transcription factors and microRNAs

Biersack¹

2020

CDR

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“…Breast cancer is the second leading cause of cancer death in females after lung cancer. The incidence of breast cancer increases with age, and more than 50 % of all women diagnosed are 65 or older.1 It is expected that by the year 2030, 20 % of the US population will be > 65 years old, and thus an ever-growing number of women will be diagnosed with this disease [5].…”

Section: Introductionmentioning

confidence: 99%

“…= 0.0100 μM convert to nM). X=CH,N; Ar=4-Cl-Ph, 4-NO 2 -Ph R=H, OCH 3 , N(CH 3 ) R=H, NO 2 ; R 1 =OCH Ph, CH 3 , Ph, 4-Cl-Ph, 4-OCH 3 -PhAnother series of hybrids, viz., 2-pyridyl hexahydrocycloocta[4,5] thieno[2,3-d] pyrimidines (compounds 27), with different substituents at the C-4 position was synthesized by Kassab and Gedawy and tested their in vitro antiproliferative activity against 60 different human tumor cell lines representing leukemia, melanoma, and cancers of the colon, central nervous system, lung, ovary, kidney, prostate including breast[31]. Commonly, compounds carrying pyridyl moiety at the C-2 position were found to have better anti-cancer activity.…”

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confidence: 99%

A Short Review on Heterocyclic Compounds Showing Anti-Breast Cancer Activity

Ayana¹,

Vijayakumar²,

Athulya³

et al. 2021

J. Sci. Res.

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Breast cancer (BC) is the most common cancer for females, and its incidence tends to increase year by year. Currently, the backbone of therapy for BC is mainly chemotherapy; however, its toxicity in normal cells and acquired tumor resistance to the drug users are considered the main barriers. Therefore, there is still an urgent need for the development of more effective and safer anti-BC agents. Based on previous reference documents in recent years, this review covers the work reported on the anti-BC compounds classified according to the structures. This review summarized significant anti-BC compounds organized by functional groups according to the animal model data, although there would be some limitations. This review highlights the properties of new compounds having promising anti-BC properties, which may be proven to be more effective and selective, and possibly free of unwanted side effects. The reviewed compounds represent an interesting possibility of overcoming BC and reducing the percentage of patients with an inadequate response to drug therapy.

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Design and synthesis of indole-based elipticine analogues as topoisomerase IIβ inhibitors

El Sayed,

Sarhan,

Alturaifi

et al. 2024

Med Chem Res

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Towards breast cancer targeting: Synthesis of tetrahydroindolocarbazoles, antibreast cancer evaluation, uPA inhibition, molecular genetic and molecular modelling studies

Cited by 8 publications

References 33 publications

3,3’-Diindolylmethane and its derivatives: nature-inspired strategies tackling drug resistant tumors by regulation of signal transduction, transcription factors and microRNAs

3,3’-Diindolylmethane and its derivatives: nature-inspired strategies tackling drug resistant tumors by regulation of signal transduction, transcription factors and microRNAs

A Short Review on Heterocyclic Compounds Showing Anti-Breast Cancer Activity

Design and synthesis of indole-based elipticine analogues as topoisomerase IIβ inhibitors

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