Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts

Kachhadia, V. V.; Rajagopal, Sridharan; Ponpandian, Thanasekaran; Radhakrishnan, Vignesh; Anandhan, Karnambaram; Prabhu, D.; Rajendran, Praveen; Nidhyanandan, Saranya; Roy, Anshu M.; Ahamed, Fakrudeen Ali; Surendran, Narayanan; Rajagopal, Sriram; Narayanan, Shridhar; Gopalan, Balasubramanian

doi:10.1016/j.ejmech.2015.11.014

Cited by 7 publications

(5 citation statements)

References 29 publications

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“…[114] Most of the 42 tested compounds showedagood HDAC inhibition (IC 50 < 100 nm)a nd good antiproliferative activity in three different cancerc ell lines (HCT-116, NCIH-460, and U251) with GI 50 ranging from 0.01 mm to 3 mm.I nF igure 11,t wo of the best vinyl hydroxamic acids (42 and 43)a re depicted as examples. [105] The mosta ctive compound 44 ( Figure 11)o fas eries of 28 (Z)-and (E)-styrylbenzoxazolones, containing 3,4,5-trimethoxystyryl fragment at position6 of benzoxazolone, showedt he highest antiproliferative effect against HepG2, EA.hy926, and K562 cancer cell lines and on additional cell lines, with IC 50 valuess imilar to or better than that of CA-4. It induced mitotic arrest in the G 2 /M phase like CA-4, as confirmed by X-ray studies.…”

Section: (Z)-stilbenesmentioning

confidence: 98%

“…Most of the 42 tested compounds showed a good HDAC inhibition (IC 50 <100 n m ) and good antiproliferative activity in three different cancer cell lines (HCT‐116, NCIH‐460, and U251) with GI 50 ranging from 0.01 μ m to 3 μ m . In Figure , two of the best vinyl hydroxamic acids ( 42 and 43 ) are depicted as examples …”

Section: Synthetic Anticancer Stilbenesmentioning

confidence: 99%

“…These compounds exhibitedt he most potent growth inhibition in the micromolar range,a gainst most of the human cancer cell lines in the panel. [104] Heteroaromatic stilbene derivatives are also hybrid molecules, [41,105] that combine the anticancer properties of the stilbene moiety with that of acounterpart with documented ability to modulate one or several pathways relevant for cancer pathogenesis. [106] Polypharmacological compounds represent an innovative strategy to obtain an ew chemical entity with multitarget activities.…”

Section: Heteroaromatic Stilbenesmentioning

confidence: 99%

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Anticancer Activity of Stilbene‐Based Derivatives

et al. 2017

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Stilbene is an abundant structural scaffold in nature, and stilbene-based compounds have been widely reported for their biological activity. Notably, (E)-resveratrol and its natural stilbene-containing derivatives have been extensively investigated as cardioprotective, potent antioxidant, anti-inflammatory, and anticancer agents. Starting from its potent chemotherapeutic activity against a wide variety of cancers, the stilbene scaffold has been subject to synthetic manipulations with the aim of obtaining new analogues with improved anticancer activity and better bioavailability. Within the last decade, the majority of new synthetic stilbene derivatives have demonstrated significant anticancer activity against a large number of cancer cell lines, depending on the type and position of substituents on the stilbene skeleton. This review focuses on the structure-activity relationship of the key compounds containing a stilbene scaffold and describes how the structural modifications affect their anticancer activity.

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Section: (Z)-stilbenesmentioning

confidence: 98%

Section: Synthetic Anticancer Stilbenesmentioning

confidence: 99%

Section: Heteroaromatic Stilbenesmentioning

confidence: 99%

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Anticancer Activity of Stilbene‐Based Derivatives

et al. 2017

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“…According to the data, 127l causes DNA damage, which leads to S-phase arrest, and eventually cell death (Table 32). Kachhadia et al 74 described the synthesis of stilbene derivatives and evaluated their anti-cancer activity. Compound 131a exhibited the highest inhibitory activity against histone deacetylase (HDAC).…”

Section: Anti-cancer Activitymentioning

confidence: 99%

“…Kachhadia et al 74 described the synthesis of stilbene derivatives and evaluated their anti-cancer activity. Compound 131a exhibited the highest inhibitory activity against histone deacetylase (HDAC).…”

Section: Anti-cancer Activitymentioning

confidence: 99%

Medicinal chemistry perspective on the structure–activity relationship of stilbene derivatives

Sepehri,

Khedmati,

Yousef-Nejad

et al. 2024

RSC Adv.

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Synthetic approaches toward stilbenes and their related structures

2017

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Compounds belonging to the stilbene family have gained remarkable significance in pharmaceutical as well as material chemistry. The current review covers the various synthetic approaches for the syntheses of stilbene scaffold and related structures over last 30 years. In addition, this review also highlights the role of stilbene intermediates used in the synthesis of important molecules with diverse applications in the field of pharmaceutics and material science.

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Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts

Cited by 7 publications

References 29 publications

Anticancer Activity of Stilbene‐Based Derivatives

Anticancer Activity of Stilbene‐Based Derivatives

Medicinal chemistry perspective on the structure–activity relationship of stilbene derivatives

Synthetic approaches toward stilbenes and their related structures

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