Tuberculosis (TB) remains among the world’s great public health challenges. Worldwide resurgence of TB is due to two major problems: the acquired immunodeficiency syndrome (AIDS) epidemic, which started in the mid-1980s, and the outbreak of multidrug resistant tuberculosis (MDR-TB). Thus, there is an urgent need for anti-TB drugs with improved properties such as: Enhanced activity against MDR strains, reduced toxicity, shortened duration of therapy, rapid mycobactericidal mechanism of action and the ability to penetrate host cells and exert antimycobacterial effects in the intracellular environment. Indoline-2,3-dione (isatin) derivatives are reported to show antitubercular activities, accordingly, isatin is a versatile lead molecule for designing of potential anti-tubercular agent. The current review outlines isatin derivatives with potential anti-tubercular activity.

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Anti-Tubercular Activity of Isatin Derivatives

Baylis–Hillman adduct-derived N-cinnamyl-substituted isatin derivatives were synthesized and evaluated for their antitubercular activity on Mycobacterium tuberculosis H37Rv strain ATCC 27294 by agar dilution method. Anticancer activity for the same compounds was also screened on four different cell lines: Chinese hamster ovary (CHO cells), Colo 205 (human colon cancer), Sup-T1 (human lymphoma) and C6 glioma (rat glioma) by MTT assay method. The compounds (3j–l) have shown significant activity against Mycobacterium strain and the compound 3l has shown specific cytotoxic activity.

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Synthesis, antitubercular and anticancer activity of new Baylis–Hillman adduct-derived N-cinnamyl-substituted isatin derivatives

Schiff bases were prepared from S-benzyldithiocarbazate with 5-fluro-, 5-chloro- and 5-bromoisatin. All are potential tridentate nitrogen, oxygen, sulfur donors. They were found to be selectively active against MCF-7 cell line (Human non-metastatic mammary gland adenocarcinoma cell line). The bromide and fluoride compounds were the most active with IC50 values of 6.40 μM (2.6 μg/mL) and 9.26 μM (3.2 μg/mL) respectively while the chloride derivative was weakly active with an IC50 value of 38.69 μM (14.0 μg/mL). The cytotoxic activity of the halo substituted isatins against the breast cancer cell lines tested is in the order of Br > F > Cl. Planarity of the isatin ring in the Schiff bases can be arranged in the following order SB5FISA > SB5ClISA > SB5BrISA while the perpendicularity of the benzyl ring towards the dithiocarbazate plane can be ordered as follows, SB5FISA > SB5BrISA > SB5ClISA. Schiff bases were prepared from S-benzyldithiocarbazate with 5-fluro-, 5-chloro- and 5-bromoisatin. They were found to be selectively active against MCF-7 cell line (Human non-metastatic mammary gland adenocarcinoma cell line) with the bromide compound was the most active with IC50 value of 6.40 μM (2.6 μg/mL).

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Synthesis, Characterization and Cytotoxic Activity of S-Benzyldithiocarbazate Schiff Bases Derived from 5-Fluoroisatin, 5-Chloroisatin, 5-Bromoisatin and Their Crystal Structures

One aspect of the invention relates to novel isatin derivative compounds and the pharmaceutical composition thereof. Another aspect of the invention relates to methods of using the isatin derivative compounds disclosed herein and the pharmaceutical compositions thereof. In certain embodiments, the method is used to treat a cancer or a tumor in a subject including, without limitation, prostate cancer, melanoma, pancreatic cancer, ovarian cancer, and lymphoma. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the activation of one or more proteins such as EGFR, Erk1/2, Her2/Neu, Jak2, Src, Stat3, Akt, Cyclin B1, and Cdc25C. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the disruption of microtubule formations.

Isatin derivatives, pharmaceutical compositions thereof, and methods of use thereof

We report herein on the synthesis of some isatin Schiff’s bases (1–11), which were prepared from the reaction of isatin and some aromatic amines. These in turn were converted to the corresponding Mannich bases (12-23) by reaction with a number of secondary amines and formaldehyde, taking advantage of the active –NH group in the isatin. The structures of these compounds were elucidated using standard spectroscopic and analytical methods.

Facile synthesis of Schiff and Mannich bases of isatin derivatives

Some compounds selected from the isatin derivatives and their metalleted products were used to study their molluscicidal effect on Biomphalaria alexandrina. The results indicated that some of these compounds showed good results and seem to be promising molluscicides.

el-Sawi Ea

Papers

Studies on the molluscicidal action of some isatin derivatives against Biomphalaria alexandrina in Egypt.