Cytotoxicity study of dimethylisatin and its heterocyclic derivatives

Hossain, Mohammad Mamun; Islam, Nazrul; Khan, Rahat; Islam, Md. Rabiul

doi:10.3329/bjp.v2i2.572

Cited by 13 publications

(10 citation statements)

References 6 publications

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“…Hence a significant rising research interest in the design of oxindoles as drugs is currently observed in the field of medicinal organic chemistry. The Schiff bases and spiro-thiadiazoline derivatives of isatins have shown remarkable biological activities, which is already reported [2][3][4] . On the other hand, the consumption of citrus fruits, vegetables, red wines, juices, etc.…”

Section: Introductionmentioning

confidence: 70%

Antioxidant potential study of some synthesized N-heterocycles

Hossain

Shaha²,

Aziz³

2009

Bangladesh Med Res Counc Bull

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Nitrogen containing heterocyclic compounds such as oxindoles especially isatins and their derivatives have excellent biological properties such as anti-inflammatory, antimicrobial, anticancer activity. In addition, this is first time ever we would like to report the antioxidant properties of the said class of compounds. To determine such an important bioactivity a number of halogenated oxindoles 1-3, their diaza-biphenyl derivatives (4-6), ring extended biphenyl (7) and bis-amide (8) were synthesized by classical heating method. The antioxidant activity of all the synthesized compounds was screened by DPPH method with respect to ascorbic acid. In our present investigation some of the synthesized compounds (1, 2, 3, 5 and 6) were found to be active.

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Section: Introductionmentioning

confidence: 70%

Antioxidant potential study of some synthesized N-heterocycles

Hossain

Shaha²,

Aziz³

2009

Bangladesh Med Res Counc Bull

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“…Increasing the number of electron-withdrawing groups on the ring to make combinations of dibromo-, tribromo-, iodo-and nitroisatin derivatives (3h-n) also enhanced the overall activity against a panel of human cancer cell lines, by up to 100-fold from that of the parent molecule (1). Despite this trend, 6,7-dimethylisatin was deemed inactive in a brine shrimp lethality assay (LD 50 96 ppm) compared to other substituted heterocyclic isatins [40], suggesting that together with substitution on the aromatic ring A, substitution at N1, C2 and/or C3, may also significantly enhance the molecule's cytotoxic effect (see sections 2.2 -…”

Section: Mono- Di-and Tri-substituted Aromatic Isatin Derivativesmentioning

confidence: 99%

Recent Highlights in the Development of Isatin-Based Anticancer Agents

Vine¹,

Matesic²,

Locke³

et al. 2013

Advances in Anticancer Agents in Medicinal Chemistry

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Isatin (1H-indole-2,3-dione) and its derivatives are responsible for a broad spectrum of biological activities. Among these the cytotoxic and antineoplastic properties have been the most widely reported. The synthetic versatility of the isatin, due to its privileged scaffold, has led to the generation of a large number of structurally diverse derivatives which include analogues derived from either mono-, di-, and trisubstitution of the aryl ring A, and/or those obtained by derivatisation of the isatin nitrogen and C2/C3 carbonyl moieties. These compounds inhibit cancer cell proliferation and tumour growth via interaction with a variety of intracellular targets such as DNA, telomerase, tubulin, P-glycoprotein, protein kinases and phosphatases. Herein we review recent highlights in the development of isatin-based compounds as anticancer agents with a particular focus on the cytotoxicity and structure activity relationships. Abstract:Isatin (1H-indole-2,3-dione) and its derivatives are responsible for a broad spectrum of biological activities. Among these the cytotoxic and antineoplastic properties have been the most widely reported. The synthetic versatility of the isatin, due to its privileged scaffold, has led to the generation of a large number of structurally diverse derivatives which include analogues derived from either mono-, di-, and tri-substitution of the aryl ring A, and/or those obtained by derivatisation of the isatin nitrogen and C2/C3 carbonyl moieties. These compounds inhibit cancer cell proliferation and tumour growth via interaction with a variety of intracellular targets such as DNA, telomerase, tubulin, Pglycoprotein, protein kinases and phosphatases. Herein we review recent highlights in the development of isatin-based compounds as anticancer agents with a particular focus on the cytotoxicity and structure activity relationships.

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“…Hence a significant rising research interest in the design of oxindoles and spirothiadiazolines as drugs is currently observed in the field of medicinal organic chemistry [7]. The conventional synthesis of the similar type Schiff-bases and thiadiazoline derivatives of isatin derivatives and their consequent biological activities have been reported in many of ours and other previous articles [8][9][10][11]. Besides, MW-assisted synthesis of isatin related compounds in different ways is also reported [11].…”

Section: Introductionmentioning

confidence: 99%

Microwave-assisted Efficient Synthesis of Isatins and <i>spiro</i>-Thiadiazolines under Green Chemistry Protocol

et al. 2010

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MW-assisted treatment of oximinoacetanilides obtained from substituted primary aromatic amines was carried out in conc. H 2 SO 4 medium for 5-10 sec to give cyclic amides (isatins) through intramolecular cyclization by means of electrophilic aromatic substitution. Isatins reacted with thiosemicarbazide under MW-condition gave the corresponding Schiff-bases. The Schiff-bases undergo cyclization in presence of minimal Ac 2 O under MW-irradiation for 3-4 min to give the spiro-thiadiazoline acetyl derivatives in excellent yield.

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Cytotoxicity study of dimethylisatin and its heterocyclic derivatives

Cited by 13 publications

References 6 publications

Antioxidant potential study of some synthesized N-heterocycles

Antioxidant potential study of some synthesized N-heterocycles

Recent Highlights in the Development of Isatin-Based Anticancer Agents

Microwave-assisted Efficient Synthesis of Isatins and <i>spiro</i>-Thiadiazolines under Green Chemistry Protocol

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