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Biomimetic and bioactive biomaterials are desirable as tissue engineering scaffolds by virtue of their capability to mimic natural environments of the extracellular matrix. Biomimeticity has been achieved by the incorporation of synthetic short peptide sequences into suitable materials either by surface modification or by bulk incorporation. Research in this area has identified several novel synthetic peptide segments, some of them with cell-specific interactions, which may serve as potential candidates for use in explicit tissue applications. This review focuses on the developments and prospective directions of incorporating short synthetic peptide sequences onto scaffolds for tissue engineering, with emphasis on the chemistry of peptide immobilization and subsequent cell responses toward modified scaffolds. The article provides a decision-tree-type flow chart indicating the most probable cellular events on a given peptide-modified scaffold along with the consolidated list of synthetic peptide sequences, supports as well as cell types used in various tissue engineering studies, and aims to serve as a quick reference guide to peptide chemists and material scientists interested in the field.

1 Microtubule binding drugs are of special interest as they have important roles in the modulation of cellular functions and many of them act as anticancer agents. 4-Amino-5-benzoyl-2-(4-methoxyphenylamino)thiazole (DAT1) was identified as one of the active compounds from a series of diaminoketothiazoles in a cell-based screening assay to discover cytotoxic compounds. 2 DAT1 shows cytotoxicity with GI 50 values ranging from 0.05 to 1 mM in different malignant cell lines with an average value of 0.35 mM. It blocks mitosis in the prometaphase and metaphase stages. In HeLa cells, DAT1 blocks the spindle function by disturbing spindle microtubule and chromosome organization. 3 The drug also inhibits assembly of brain microtubules and binds tubulin specifically at a single site with induction of fluorescence. The dissociation constant of DAT1 binding to tubulin was determined as 2.971 mM at 241C. The binding site of DAT1 on tubulin overlaps with that of the conventional colchicine-binding site. 4 DAT1 can thus be considered as a lead compound of a new class of small molecules and this study can be used as a step to develop potent antimitotic agents for the control of cytoskeletal functions and cell proliferation. It would also be an interesting probe for the structure-function studies of tubulinmicrotubule system.

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Probing the chemical space of luminescent organic materials built on novel cores is highly imperative for its potential to expand the horizons of advanced functional materials. Small organic fluorophores possessing therapeutic traits can contribute to theranostics. We coupled computational and classical synthetic chemistry strategies for the rational design of 5-(hetero-2-yl)-1,3-thiazoles as color-tunable fluorophore core. With the aid of DFT and TD-DFT, we prove that the multi-heterocyclic system is built on a thiazole-het core with three inherent tunable sites on thiazole (C2, C4, and C5) capable of accommodating a panoply of substituents as a multifunctional molecular materials' platform. This de novo design offered unprecedented freedom to control strength and direction of charge transfer by varying donor-acceptor fragments. A 30-member fluorophore library built on thiazole-thiophene/furan core was accomplished using commercial reagents by a simple [4 + 1] synthesis. Structure-photophysical property studies revealed large Stokes shift, positive solvatochromism, acidochromism, and color tunability in different solvents and were rationalized using computational calculations. In vitro studies indicated 1a to be active against HL-60 cell lines, suggesting the possibility of expanding the core for theranostics. The lower values of computed hole reorganization energies indicated their potential as hole transporting materials in optoelectronics and widen the scope of these molecules as advanced functional materials.