The natural products served as an invaluable resource in the investigation for potential agents of therapeutic value. Recently approved drugs are natural products themselves or modified natural products. An accepted strategy for the design of novel compounds is to improve the biologically relevance compound by innovatively modulate a part of the structural motifs of already identified lead compounds. Recently it was found that simple modification of drug molecules enhances the activities of the drugs. For example, simplified analogue of natural anguinomycins C is (Z)-3-ethyl-5-methylhexa-1,3-diene substituted 5,6-dihydro-2H-pyran-2-ones which lack of polyketide side chain.
Fluoro-vinyl compounds exhibit an important role in biological sciences as peptidomimics and enzyme inhibitors and are also key synthons for various organic synthetic transformations. In addition to thatstereospecific substitution of fluorine to acrylates imparts significant biological activity in chemistry of pheromones including drugs. Fluoro-polyenes are of much current interest as they are important for the treatment of dermatologic diseases and cancers. In addition to that they are important building blocks for the synthesis of different biologically active molecules and new fluorinated materials such as crosslinkable dendrimers.
Incorporation of fluorine into organic molecule changes the conformation to a substantial extent. Fluorine at 6-position of BaP (6-F-BaP) changes the conformation of the tetrahydro ring of the corresponding DEs as well as dihydrodiol (DHD). The (R,S,S,R)-diol epoxide isomer of 6-F-BaP as well as its metabolic precursor DHD showed quasi-diaxial orientation ofvicinal hydroxyl groups and showed no tumorigenic activity.
Free radical reaction is an important tool in modern synthesis for construction of cyclic ethers including bioactive molecules. Titanocene (III) chloride efficiently generate metal centred radical which subsequently accepted by alkene or alkyne either via intra-molecularly or inter-molecularly to form cyclic or acyclic compound respectively. Similarly active bromo-compound like alpha-bromo carbonyl compound or allyl, benzyl bromide produces radical in presence of Titanocene (III) chloride and subsequently accepted by alkene or alkyne either via intra-molecularly or inter-molecularly to form cyclic or acyclic compound respectively.